bace-1 inhibitors Search Results


chromane-based spirocyclic acyl guanidine-derived bace-1 inhibitors  (Array BioPharma)
90
Array BioPharma chromane-based spirocyclic acyl guanidine-derived bace-1 inhibitors
<t>Chromane-based</t> spirocyclic acyl guanidine-derived BACE-1 inhibitor 21 develop by <t>Array</t> <t>BioPharma</t> together with Genentech .
Chromane Based Spirocyclic Acyl Guanidine Derived Bace 1 Inhibitors, supplied by Array BioPharma, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Average 90 stars, based on 1 article reviews
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bace1 inhibitor mk-8931  (Forum pharmaceuticals)
90
Forum pharmaceuticals bace1 inhibitor mk-8931
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Bace1 Inhibitor Mk 8931, supplied by Forum pharmaceuticals, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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bace-1 inhibitors  (MultiTarget Pharmaceuticals)
90
MultiTarget Pharmaceuticals bace-1 inhibitors
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Bace 1 Inhibitors, supplied by MultiTarget Pharmaceuticals, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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om99-2 h-5108  (Bachem)
90
Bachem om99-2 h-5108
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Om99 2 H 5108, supplied by Bachem, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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gl189  (Merck KGaA)
90
Merck KGaA gl189
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Gl189, supplied by Merck KGaA, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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bace1 inhibitor  (Future Medicine Ltd)
90
Future Medicine Ltd bace1 inhibitor
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Bace1 Inhibitor, supplied by Future Medicine Ltd, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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sterol-linked bace1 inhibitors  (JADO Technologies GmbH)
90
JADO Technologies GmbH sterol-linked bace1 inhibitors
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Sterol Linked Bace1 Inhibitors, supplied by JADO Technologies GmbH, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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bace1 inhibitor (bacei)  (Axon Medchem LLC)
90
Axon Medchem LLC bace1 inhibitor (bacei)
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Bace1 Inhibitor (Bacei), supplied by Axon Medchem LLC, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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pharmacophore hypothesis for bace-1 inhibitors  (Hypogen Inc)
90
Hypogen Inc pharmacophore hypothesis for bace-1 inhibitors
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Pharmacophore Hypothesis For Bace 1 Inhibitors, supplied by Hypogen Inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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bace1  (Biomol GmbH)
90
Biomol GmbH bace1
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Bace1, supplied by Biomol GmbH, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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bace1 inhibitor atabecestat  (Shionogi)
86
Shionogi bace1 inhibitor atabecestat
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
Bace1 Inhibitor Atabecestat, supplied by Shionogi, used in various techniques. Bioz Stars score: 86/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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bace1 inhibitor  (Georg Thieme Verlag KG)
90
Georg Thieme Verlag KG bace1 inhibitor
<t>BACE1</t> inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).
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Image Search Results


Chromane-based spirocyclic acyl guanidine-derived BACE-1 inhibitor 21 develop by Array BioPharma together with Genentech .

Journal: Pharmaceuticals

Article Title: BACE-1 and γ-Secretase as Therapeutic Targets for Alzheimer’s Disease

doi: 10.3390/ph12010041

Figure Lengend Snippet: Chromane-based spirocyclic acyl guanidine-derived BACE-1 inhibitor 21 develop by Array BioPharma together with Genentech .

Article Snippet: Array BioPharma together with Genentech developed a series of chromane-based spirocyclic acyl guanidine-derived BACE-1 inhibitors leading to compound 21 ( ).

Techniques: Derivative Assay

BACE1 inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).

Journal: Frontiers in Aging Neuroscience

Article Title: BACE1 Inhibitor MK-8931 Alters Formation but Not Stability of Dendritic Spines

doi: 10.3389/fnagi.2018.00229

Figure Lengend Snippet: BACE1 inhibitor MK-8931 altered plasticity of dendritic spines in vivo . (A) Micrographs of eGFP-labeled apical dendrites of layer V pyramidal neurons in somatosensory cortex before, during and after administration of vehicle or MK-8931. Treatment started 8 days after first imaging timepoint and was continued over 21 days, every 12 h. White arrowheads exemplarily mark representative spines which were stable over the entire imaging period. Newly gained spines are labeled with green arrowheads and lost spines are labeled with magenta arrowheads. (B) Quantification of spine density (C,D) fraction of gained and lost spines in mice treated with vehicle or MK-8931 (20 mg/kg). N = 5 animals per group, n = 10 dendrites per animal. Data is presented as mean ± SEM. Bonferroni post-hoc test results: * p < 0.05, ** p < 0.01, *** p < 0.001, **** p < 0.0001 from two-way ANOVA (day 0–28).

Article Snippet: The BACE1 inhibitor MK-8931 was synthesized following the schemes provided by FORUM Pharmaceuticals (Waltham, MA, USA) and formulated in 10% (w/v) 2-hydroxypropyl-beta-cyclodextrin.

Techniques: In Vivo, Labeling, Imaging

MK-8931 treatment did not cause spine elimination. (A) Spine stability and turnover rates in vehicle and MK-8931 treated mice. Daily turnover rate significantly decreased at the end of inhibitor treatment. (B,C) MK-8931 treatment significantly decreased density of transient spines, whereas density of stable spines was not affected. Bonferroni post-hoc test: ns: p = 0.4926, * p < 0.05, *** p < 0.001, **** p < 0.0001 (two-way ANOVA between day 0–28). (D) Survival rate of newly gained spines was not affected by BACE1 inhibitor treatment. N = 5 animals per group, n = 10 dendrites per animal. Two-tailed Student’s t -test, t (8) = 0.9, p = 0.394. Data presented as mean ± SEM.

Journal: Frontiers in Aging Neuroscience

Article Title: BACE1 Inhibitor MK-8931 Alters Formation but Not Stability of Dendritic Spines

doi: 10.3389/fnagi.2018.00229

Figure Lengend Snippet: MK-8931 treatment did not cause spine elimination. (A) Spine stability and turnover rates in vehicle and MK-8931 treated mice. Daily turnover rate significantly decreased at the end of inhibitor treatment. (B,C) MK-8931 treatment significantly decreased density of transient spines, whereas density of stable spines was not affected. Bonferroni post-hoc test: ns: p = 0.4926, * p < 0.05, *** p < 0.001, **** p < 0.0001 (two-way ANOVA between day 0–28). (D) Survival rate of newly gained spines was not affected by BACE1 inhibitor treatment. N = 5 animals per group, n = 10 dendrites per animal. Two-tailed Student’s t -test, t (8) = 0.9, p = 0.394. Data presented as mean ± SEM.

Article Snippet: The BACE1 inhibitor MK-8931 was synthesized following the schemes provided by FORUM Pharmaceuticals (Waltham, MA, USA) and formulated in 10% (w/v) 2-hydroxypropyl-beta-cyclodextrin.

Techniques: Two Tailed Test