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irosustat (MedChemExpress)

Name: irosustat
Brand: MedChemExpress
Rating: 94 (2 reviews)

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MedChemExpress irosustat

( A to H ) Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on TCPS with indicated doses of (A) Y-27632, (B) LY294002, (C) H1152, (D) SB203580, (E) <t>irosustat,</t> (F) TM5441, (G) losartan, and (H) SD-208. ( I ) Heatmap showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data are plotted as means ± SEM ( N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t test with Welch’s correction and indicated as * P < 0.05 (Y-27632 and losartan showed a significant difference in efficacy between male and female VICs).

Irosustat, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 94/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 94 stars, based on 2 article reviews

irosustat - by Bioz Stars, 2026-02

94/100 stars

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1) Product Images from "Determining sex differences in aortic valve myofibroblast responses to drug combinations identified using a digital medicine platform"

Article Title: Determining sex differences in aortic valve myofibroblast responses to drug combinations identified using a digital medicine platform

Journal: Science Advances

doi: 10.1126/sciadv.adu2695

Figure Legend Snippet: ( A to H ) Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on TCPS with indicated doses of (A) Y-27632, (B) LY294002, (C) H1152, (D) SB203580, (E) irosustat, (F) TM5441, (G) losartan, and (H) SD-208. ( I ) Heatmap showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data are plotted as means ± SEM ( N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t test with Welch’s correction and indicated as * P < 0.05 (Y-27632 and losartan showed a significant difference in efficacy between male and female VICs).

Techniques Used: Cell Culture, Generated, Two Tailed Test

( A to H ) Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on stiff hydrogels with indicated doses of (A) Y-27632, (B) LY294002, (C) H1152, (D) SB203580, (E) irosustat, (F) TM5441, (G) losartan, and (H) SD-208. ( I ) Heatmap showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data are plotted as means ± SEM ( N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t test with Welch’s correction and indicated as * P < 0.05 (losartan showed a significant difference in efficacy between male and female VICs).

Figure Legend Snippet: ( A to H ) Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on stiff hydrogels with indicated doses of (A) Y-27632, (B) LY294002, (C) H1152, (D) SB203580, (E) irosustat, (F) TM5441, (G) losartan, and (H) SD-208. ( I ) Heatmap showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data are plotted as means ± SEM ( N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t test with Welch’s correction and indicated as * P < 0.05 (losartan showed a significant difference in efficacy between male and female VICs).

Techniques Used: Cell Culture, Generated, Two Tailed Test

( A ) Percent αSMA reduction in male VICs cultured with IDentif.AI-designed effective (green) and ineffective (red) drug combinations. (1) indicates L1 dose and (2) indicates L2 dose of that drug ( n = 3 to 4). The percent αSMA reduction for monotherapies at L1/L2 doses is summarized in table S6. ( B ) Correlation plot between the predicted versus measured percent αSMA reduction for IDentif.AI-designed combinations. ( C ) Validation of top three and bottom ranked IDentif.AI drug combinations ( N = 3). ( D ) Representative immunofluorescent images with αSMA stained in green and DAPI stained in blue. Scale bars, 100 μm. ( E ) Interaction map of Losartan and SD-208 at various dose ratios and their respective percent αSMA reduction ( N = 3). ( F ) Synergy map of losartan and SD-208 at various dose ratios ( N = 3). The black box indicates the therapeutic dosing range (0 - L2) used for IDentif.AI analysis. Statistical significance was determined by a one-sample t test against a theoretical mean of zero to represent the vehicle control and indicated as * P < 0.05, ** P < 0.01, and *** P < 0.001. Bliss synergy scores of <−10, between −10 and 10, and >10 represent antagonistic, additive, and synergistic drug interactions. Data are plotted as means ± SD. H1152, H11; irosustat, Iro; losartan, Los; LY294002, LY; SB203580, SB; SD-208, SD; TM5441, TM; Y-27632, Y27. N = number of biological replicates. n = number of gels. ns, not significant.

Figure Legend Snippet: ( A ) Percent αSMA reduction in male VICs cultured with IDentif.AI-designed effective (green) and ineffective (red) drug combinations. (1) indicates L1 dose and (2) indicates L2 dose of that drug ( n = 3 to 4). The percent αSMA reduction for monotherapies at L1/L2 doses is summarized in table S6. ( B ) Correlation plot between the predicted versus measured percent αSMA reduction for IDentif.AI-designed combinations. ( C ) Validation of top three and bottom ranked IDentif.AI drug combinations ( N = 3). ( D ) Representative immunofluorescent images with αSMA stained in green and DAPI stained in blue. Scale bars, 100 μm. ( E ) Interaction map of Losartan and SD-208 at various dose ratios and their respective percent αSMA reduction ( N = 3). ( F ) Synergy map of losartan and SD-208 at various dose ratios ( N = 3). The black box indicates the therapeutic dosing range (0 - L2) used for IDentif.AI analysis. Statistical significance was determined by a one-sample t test against a theoretical mean of zero to represent the vehicle control and indicated as * P < 0.05, ** P < 0.01, and *** P < 0.001. Bliss synergy scores of <−10, between −10 and 10, and >10 represent antagonistic, additive, and synergistic drug interactions. Data are plotted as means ± SD. H1152, H11; irosustat, Iro; losartan, Los; LY294002, LY; SB203580, SB; SD-208, SD; TM5441, TM; Y-27632, Y27. N = number of biological replicates. n = number of gels. ns, not significant.

Techniques Used: Cell Culture, Biomarker Discovery, Staining, Control

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Journal: Science Advances

Article Title: Determining sex differences in aortic valve myofibroblast responses to drug combinations identified using a digital medicine platform

doi: 10.1126/sciadv.adu2695

Figure Lengend Snippet: ( A to H ) Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on TCPS with indicated doses of (A) Y-27632, (B) LY294002, (C) H1152, (D) SB203580, (E) irosustat, (F) TM5441, (G) losartan, and (H) SD-208. ( I ) Heatmap showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data are plotted as means ± SEM ( N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t test with Welch’s correction and indicated as * P < 0.05 (Y-27632 and losartan showed a significant difference in efficacy between male and female VICs).

Article Snippet: Lyophilized drug powders were resuspended with sterile filtered deionized water [H-1152 (Tocris) and Y-27632 (Tocris)] or sterile DMSO [LY-294002 (Cell Signaling Technology), SB203580 (Selleck Chemicals), Irosustat (Selleck Chemicals), TM-5441 (MedChemExpress), SD-208 (Sigma-Aldrich), losartan (Selleck Chemicals), ibrutinib (Selleck Chemicals), bosentan (Sigma-Aldrich), and KDOAM-25 (MedChemExpress)].

Techniques: Cell Culture, Generated, Two Tailed Test

Journal: Science Advances

Article Title: Determining sex differences in aortic valve myofibroblast responses to drug combinations identified using a digital medicine platform

doi: 10.1126/sciadv.adu2695

Figure Lengend Snippet: ( A to H ) Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on stiff hydrogels with indicated doses of (A) Y-27632, (B) LY294002, (C) H1152, (D) SB203580, (E) irosustat, (F) TM5441, (G) losartan, and (H) SD-208. ( I ) Heatmap showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data are plotted as means ± SEM ( N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t test with Welch’s correction and indicated as * P < 0.05 (losartan showed a significant difference in efficacy between male and female VICs).

Techniques: Cell Culture, Generated, Two Tailed Test

Journal: Science Advances

Article Title: Determining sex differences in aortic valve myofibroblast responses to drug combinations identified using a digital medicine platform

doi: 10.1126/sciadv.adu2695

Figure Lengend Snippet: ( A ) Percent αSMA reduction in male VICs cultured with IDentif.AI-designed effective (green) and ineffective (red) drug combinations. (1) indicates L1 dose and (2) indicates L2 dose of that drug ( n = 3 to 4). The percent αSMA reduction for monotherapies at L1/L2 doses is summarized in table S6. ( B ) Correlation plot between the predicted versus measured percent αSMA reduction for IDentif.AI-designed combinations. ( C ) Validation of top three and bottom ranked IDentif.AI drug combinations ( N = 3). ( D ) Representative immunofluorescent images with αSMA stained in green and DAPI stained in blue. Scale bars, 100 μm. ( E ) Interaction map of Losartan and SD-208 at various dose ratios and their respective percent αSMA reduction ( N = 3). ( F ) Synergy map of losartan and SD-208 at various dose ratios ( N = 3). The black box indicates the therapeutic dosing range (0 - L2) used for IDentif.AI analysis. Statistical significance was determined by a one-sample t test against a theoretical mean of zero to represent the vehicle control and indicated as * P < 0.05, ** P < 0.01, and *** P < 0.001. Bliss synergy scores of <−10, between −10 and 10, and >10 represent antagonistic, additive, and synergistic drug interactions. Data are plotted as means ± SD. H1152, H11; irosustat, Iro; losartan, Los; LY294002, LY; SB203580, SB; SD-208, SD; TM5441, TM; Y-27632, Y27. N = number of biological replicates. n = number of gels. ns, not significant.

Techniques: Cell Culture, Biomarker Discovery, Staining, Control

a-h, Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on TCPS with indicated doses of a Y-27632, b LY294002, c H1152, d SB203580, e Irosustat, f TM5441, g Losartan, and h SD-208. i, Heat map showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data is plotted as mean ± standard error of the mean (N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t-test with Welch’s correction and indicated as *=P<0.05.

Journal: bioRxiv

Article Title: Determining sex differences in drug combinations targeting aortic valve myofibroblast activation using an artificial intelligence derived platform

doi: 10.1101/2024.10.02.615251

Figure Lengend Snippet: a-h, Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on TCPS with indicated doses of a Y-27632, b LY294002, c H1152, d SB203580, e Irosustat, f TM5441, g Losartan, and h SD-208. i, Heat map showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data is plotted as mean ± standard error of the mean (N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t-test with Welch’s correction and indicated as *=P<0.05.

Article Snippet: Lyophilized drug powders were resuspended with sterile filtered deionized water (H-1152 (Tocris) and Y-27632 (Tocris)) or sterile DMSO (LY-294002 (Cell Signaling Technology), SB203580 (Selleck Chemicals), Irosustat (Selleck Chemicals), TM-5441 (MedChemExpress), SD-208 (Sigma), Losartan (Selleck Chemicals), Ibrutinib (Selleck Chemicals), Bosentan (Sigma), and KDOAM-25 (MedChemExpress)).

Techniques: Cell Culture, Generated, Two Tailed Test

a-h, Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on stiff hydrogels with indicated doses of a Y-27632, b LY294002, c H1152, d SB203580, e Irosustat, f TM5441, g Losartan, and h SD-208. i, Heat map showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data is plotted as mean ± standard error of the mean (N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t-test with Welch’s correction and indicated as *=P<0.05.

Journal: bioRxiv

Article Title: Determining sex differences in drug combinations targeting aortic valve myofibroblast activation using an artificial intelligence derived platform

doi: 10.1101/2024.10.02.615251

Figure Lengend Snippet: a-h, Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on stiff hydrogels with indicated doses of a Y-27632, b LY294002, c H1152, d SB203580, e Irosustat, f TM5441, g Losartan, and h SD-208. i, Heat map showing the log ratio of male EC 20 to female EC 20 for each inhibitor. Data is plotted as mean ± standard error of the mean (N = 3 biological replicates). The best fit line shown was generated using a nonlinear regression curve fit with GraphPad Prism. Statistical significance was determined by an unpaired two-tailed t-test with Welch’s correction and indicated as *=P<0.05.

Techniques: Cell Culture, Generated, Two Tailed Test

Journal: bioRxiv

Article Title: Determining sex differences in drug combinations targeting aortic valve myofibroblast activation using an artificial intelligence derived platform

doi: 10.1101/2024.10.02.615251

Figure Lengend Snippet: a, Percent αSMA reduction in male VICs cultured with IDentif.AI-designed effective (green) and ineffective (red) drug combinations. (1) indicates L1 dose and (2) indicates L2 dose of that drug (n = 3-4). b, Correlation plot between the predicted vs measured percent αSMA reduction for IDentif.AI designed combinations. c, Validation of top three and bottom ranked IDentif.AI drug combinations (N = 3). d, Representative immunofluorescent images with αSMA stained in green and DAPI stained in blue. Scale bar = 100 μm. e, Interaction map of Losartan and SD-208 at various dose ratios and their respective percent αSMA reduction (N = 3). f, Synergy map of Losartan and SD-208 at various dose ratios (N = 3). The black box indicates the therapeutic dosing range (0 - L2) used for IDentif.AI analysis. Statistical significance was determined by a one sample t-test against a theoretical mean of zero and indicated as *=P<0.05, **=P<0.01, and ***=P<0.001. Bliss synergy scores of < -10, between -10 and 10, and > 10 represent antagonistic, additive, and synergistic drug interactions. Data is plotted as mean ± standard deviation. Abbreviations: H1152 (H11); Irosustat (Iro); Losartan (Los); LY294002 (LY); SB203580 (SB); SD-208 (SD); TM5441 (TM); Y-27632 (Y27). N = number of biological replicates. n = number of gels.

Techniques: Cell Culture, Biomarker Discovery, Staining, Standard Deviation

a, Percent αSMA reduction in female VICs cultured with IDentif.AI-designed effective (green) and ineffective (red) drug combinations. (1) indicates L1 dose and (2) indicates L2 dose of that drug (n = 4). b, Correlation plot between the predicted vs measured percent αSMA reduction for IDentif.AI designed combinations. c, Validation of top three and bottom ranked IDentif.AI drug combinations (N = 3). d, Representative immunofluorescent images with αSMA stained in green and DAPI stained in blue. Scale bar = 100 μm. e, Interaction map of LY294002 and H1152 at various dose ratios and their respective percent αSMA reduction (N = 3). f, Synergy map of LY294002 and H1152 at various dose ratios (N=3). The black box indicates the therapeutic dosing range (0 - L2) used for IDentif.AI analysis. Statistical significance was determined by a one sample t-test against a theoretical mean of zero and indicated as *=P<0.05, **=P<0.01, and ***=P<0.001. Bliss synergy scores of < -10, between -10 and 10, and > 10 represent antagonistic, additive, and synergistic drug interactions. Data is plotted as mean ± standard deviation. Abbreviations: H1152 (H11); Irosustat (Iro); Losartan (Los); LY294002 (LY); SB203580 (SB); SD-208 (SD); TM5441 (TM); Y-27632 (Y27). N = number of biological replicates. n = number of gels.

Journal: bioRxiv

Article Title: Determining sex differences in drug combinations targeting aortic valve myofibroblast activation using an artificial intelligence derived platform

doi: 10.1101/2024.10.02.615251

Figure Lengend Snippet: a, Percent αSMA reduction in female VICs cultured with IDentif.AI-designed effective (green) and ineffective (red) drug combinations. (1) indicates L1 dose and (2) indicates L2 dose of that drug (n = 4). b, Correlation plot between the predicted vs measured percent αSMA reduction for IDentif.AI designed combinations. c, Validation of top three and bottom ranked IDentif.AI drug combinations (N = 3). d, Representative immunofluorescent images with αSMA stained in green and DAPI stained in blue. Scale bar = 100 μm. e, Interaction map of LY294002 and H1152 at various dose ratios and their respective percent αSMA reduction (N = 3). f, Synergy map of LY294002 and H1152 at various dose ratios (N=3). The black box indicates the therapeutic dosing range (0 - L2) used for IDentif.AI analysis. Statistical significance was determined by a one sample t-test against a theoretical mean of zero and indicated as *=P<0.05, **=P<0.01, and ***=P<0.001. Bliss synergy scores of < -10, between -10 and 10, and > 10 represent antagonistic, additive, and synergistic drug interactions. Data is plotted as mean ± standard deviation. Abbreviations: H1152 (H11); Irosustat (Iro); Losartan (Los); LY294002 (LY); SB203580 (SB); SD-208 (SD); TM5441 (TM); Y-27632 (Y27). N = number of biological replicates. n = number of gels.

Techniques: Cell Culture, Biomarker Discovery, Staining, Standard Deviation

a, Bar plot and b correlation plot of percent αSMA reduction difference (male-female) between male and female VICs cultured with top predicted male-biased and female-biased combinations. (1) indicates L1 dose and (2) indicates L2 dose of that drug (N = 3). c, Percent αSMA reduction difference between male and female VICs cultured with groups of predicted male-biased and female-biased combinations with three distinct drug combinations per group. d,e, Quantitative RT-qPCR of relative d ACTA2 and e COL1A1 gene expression in male and female VICs (n = 6-8). f, Bliss synergy scores for male and female VICs cultured with identified male synergistic dose ratios of Losartan and SD-208 on stiff hydrogels (n = 3-4). g, Bliss synergy scores for male and female VICs cultured with identified female synergistic dose ratios of LY294002 and H1152 on stiff hydrogels (n = 3-4). h, Bliss synergy scores for male and female VICs cultured with one of three male synergistic dose ratios of Losartan/SD-208 or one of three female synergistic dose ratios of LY294002/H1152. Statistical significance was determined for a by one sample t-test against a theoretical mean of zero, c and h by unpaired two-tailed t-test with Welch’s correction, and d-g by one-way ANOVA with Tukey posttests. For all graphs, significance between groups is indicated as *=P<0.05 and ****=P<0.0001 Significance relative to male control is indicated as ####=P<0.001 and significance relative to female control is indicated as $$=P<0.01 and $$$$=P<0.001. Bliss synergy scores of < -10, between -10 and 10, and > 10 represent antagonistic, additive, and synergistic drug interactions. Data is plotted as mean ± standard deviation. Abbreviations: Irosustat (Iro); Losartan (Los); LY294002 (LY); SB203580 (SB); SD-208 (SD); TM5441 (TM); Y-27632 (Y27). N = number of biological replicates. n = number of gels.

Journal: bioRxiv

Article Title: Determining sex differences in drug combinations targeting aortic valve myofibroblast activation using an artificial intelligence derived platform

doi: 10.1101/2024.10.02.615251

Figure Lengend Snippet: a, Bar plot and b correlation plot of percent αSMA reduction difference (male-female) between male and female VICs cultured with top predicted male-biased and female-biased combinations. (1) indicates L1 dose and (2) indicates L2 dose of that drug (N = 3). c, Percent αSMA reduction difference between male and female VICs cultured with groups of predicted male-biased and female-biased combinations with three distinct drug combinations per group. d,e, Quantitative RT-qPCR of relative d ACTA2 and e COL1A1 gene expression in male and female VICs (n = 6-8). f, Bliss synergy scores for male and female VICs cultured with identified male synergistic dose ratios of Losartan and SD-208 on stiff hydrogels (n = 3-4). g, Bliss synergy scores for male and female VICs cultured with identified female synergistic dose ratios of LY294002 and H1152 on stiff hydrogels (n = 3-4). h, Bliss synergy scores for male and female VICs cultured with one of three male synergistic dose ratios of Losartan/SD-208 or one of three female synergistic dose ratios of LY294002/H1152. Statistical significance was determined for a by one sample t-test against a theoretical mean of zero, c and h by unpaired two-tailed t-test with Welch’s correction, and d-g by one-way ANOVA with Tukey posttests. For all graphs, significance between groups is indicated as *=P<0.05 and ****=P<0.0001 Significance relative to male control is indicated as ####=P<0.001 and significance relative to female control is indicated as $$=P<0.01 and $$$$=P<0.001. Bliss synergy scores of < -10, between -10 and 10, and > 10 represent antagonistic, additive, and synergistic drug interactions. Data is plotted as mean ± standard deviation. Abbreviations: Irosustat (Iro); Losartan (Los); LY294002 (LY); SB203580 (SB); SD-208 (SD); TM5441 (TM); Y-27632 (Y27). N = number of biological replicates. n = number of gels.

Techniques: Cell Culture, Quantitative RT-PCR, Gene Expression, Two Tailed Test, Control, Standard Deviation

Overview of the trials registered in the database Clinical Trials ( ClinicalTrails.gov ) for the use of aromatase, STS and HSD17B1 inhibitors in breast, endometrial, ovarian, prostate cancers and endometriosis.

Journal: Frontiers in Pharmacology

Article Title: Targeting the formation of estrogens for treatment of hormone dependent diseases–current status

doi: 10.3389/fphar.2023.1155558

Figure Lengend Snippet: Overview of the trials registered in the database Clinical Trials ( ClinicalTrails.gov ) for the use of aromatase, STS and HSD17B1 inhibitors in breast, endometrial, ovarian, prostate cancers and endometriosis.

Article Snippet: Breast Cancer , NCT01840488 , , BN83495 Phase I in Post-menopausal Women , , Completed , no , Irosustat (BN83495) , Ipsen.

Techniques: Clinical Proteomics, Adjuvant, Drug discovery, Formulation

Effect of breast cancer drugs on MCF-7 Spheroid. 10 μ M of drugs was used for the treatment. MCF-7 spheroid was treated after 1 day of spheroid development. CON = ethanol control, STX = STX64 (Irosustat), QUE = quercetin, TAM = tamoxifen.

Journal: Journal of cancer therapy

Article Title: Breast Cancer MCF-7 Cell Spheroid Culture for Drug Discovery and Development

doi: 10.4236/jct.2022.133009

Figure Lengend Snippet: Effect of breast cancer drugs on MCF-7 Spheroid. 10 μ M of drugs was used for the treatment. MCF-7 spheroid was treated after 1 day of spheroid development. CON = ethanol control, STX = STX64 (Irosustat), QUE = quercetin, TAM = tamoxifen.

Article Snippet: STX64 (STX, Irosustat, Cat. No BD767626) was ordered from BLD Pharmatech Co., Limited.

Techniques: Control

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