avoralstat Search Results


avoralstat  (MedChemExpress)
94
MedChemExpress avoralstat
(a) TMPRSS2-S1P structural model ligand-binding sub-pockets (S1’, S1, S2, S3, S4, S5). (b) Docking scores of compounds curated from 3DPhyloFold and (c) correlation between algorithms. Potential inhibitors clustered around the natural S2’-peptide motif. ( d) TMPRSS2 inhibition by 3DPhyloFold compounds. (e) IC 50 value selectivity profile against S1- and SARS-CoV-2-related proteases. (f) <t>Avoralstat</t> selectivity against 70 proteases. Top row - Cα-RMSD of pairwise-structural-alignments to TMPRSS2. (g) Protease inhibition by Avoralstat correlates with 3DPhyloFold prediction. (h) TMPRSS2-S1P domain inhibition. IC 50 data represent mean ± SEM; n=3.
Avoralstat, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/avoralstat/Avoralstat/bio_rxiv__2021__01__04__425289-206-25-26
Average 94 stars, based on 1 article reviews
avoralstat - by Bioz Stars, 2026-10
94/100 stars
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avoralstat  (MuseChem Chemicals)
N/A
Avoralstat (Cat No.:I003342) is an orally bioavailable small-molecule inhibitor of plasma kallikrein (PKK) developed for prophylaxis of hereditary angioedema (HAE) due to C1 inhibitor deficiency. By blocking kallikrein activity, it is designed to reduce bradykinin
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avoralstat  (BioCryst Inc)
90
BioCryst Inc avoralstat
Treatments for C1-INH HAE under research.
Avoralstat, supplied by BioCryst Inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/avoralstat/avoralstat/pmc06788388-15-0-3
Average 90 stars, based on 1 article reviews
avoralstat - by Bioz Stars, 2026-10
90/100 stars
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avoralstat  (Biosynth Carbosynth)
N/A
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avoralstat  (Aladdin Scientific Corporation)
N/A
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avoralstat  (TargetMol)
N/A
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avoralstat  (BOC Sciences)
N/A
Avoralstat, also known as BCX-4161, is an oral plasma kallikrein (PKK) inhibitor and Bradykinin inhibitor, used to treat hereditary angioedema.
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Image Search Results


(a) TMPRSS2-S1P structural model ligand-binding sub-pockets (S1’, S1, S2, S3, S4, S5). (b) Docking scores of compounds curated from 3DPhyloFold and (c) correlation between algorithms. Potential inhibitors clustered around the natural S2’-peptide motif. ( d) TMPRSS2 inhibition by 3DPhyloFold compounds. (e) IC 50 value selectivity profile against S1- and SARS-CoV-2-related proteases. (f) Avoralstat selectivity against 70 proteases. Top row - Cα-RMSD of pairwise-structural-alignments to TMPRSS2. (g) Protease inhibition by Avoralstat correlates with 3DPhyloFold prediction. (h) TMPRSS2-S1P domain inhibition. IC 50 data represent mean ± SEM; n=3.

Journal: bioRxiv

Article Title: TMPRSS2 structure-phylogeny repositions Avoralstat for SARS-CoV-2 prophylaxis in mice

doi: 10.1101/2021.01.04.425289

Figure Lengend Snippet: (a) TMPRSS2-S1P structural model ligand-binding sub-pockets (S1’, S1, S2, S3, S4, S5). (b) Docking scores of compounds curated from 3DPhyloFold and (c) correlation between algorithms. Potential inhibitors clustered around the natural S2’-peptide motif. ( d) TMPRSS2 inhibition by 3DPhyloFold compounds. (e) IC 50 value selectivity profile against S1- and SARS-CoV-2-related proteases. (f) Avoralstat selectivity against 70 proteases. Top row - Cα-RMSD of pairwise-structural-alignments to TMPRSS2. (g) Protease inhibition by Avoralstat correlates with 3DPhyloFold prediction. (h) TMPRSS2-S1P domain inhibition. IC 50 data represent mean ± SEM; n=3.

Article Snippet: Inhibition experiments were carried out in the presence of 50 μM Cbz-GGR-AMC in the presence 10 to 500 μM compound: Camostat (Sigma-Aldrich; Cat. # SML0057), Avoralstat (MedChemExpress; Cat. # HY-16735), PCI-27483 (Cayman Chemical; Item #21334), Antipain (Sigma-Aldrich; Product #A6191), Leupeptin (Sigma-Aldrich; Product #L2884), MDL-28170 (Sigma-Aldrich; Product #M6690), Ritonavir (Sigma-Aldrich; Product #SML0491), or 5% DMSO (as a negative control).

Techniques: Ligand Binding Assay, Inhibition

(a) HEK-cells treated with Camostat, Avoralstat, PCI-27483, Antipain, or SBTI 2-hr before TMPRSS2 transfection. TMPRSS2 reduced autoproteolysis (increased TMPRSS2-FL signal; *p<0.0332, **p<0.0021, ***p<0.0002). Calu-3-cells were treated with compounds and inoculated with pseudovirions harboring (b) VSV-G or (c) SARS-CoV-2-spike-protein. Calu-3 cells were treated with (d) 100 μM or (e) indicated concentrations of each compound, then incubated with SARS-CoV-2. Viral gRNA was measured after 24-hrs. Data represent mean ± SEM; n=3. (d) Compounds reduced viral signal at 100 μM (****p<0.0001). (e) Viral signal was reduced beginning from 100 nM (*p<0.0332, ****p<0.0001).

Journal: bioRxiv

Article Title: TMPRSS2 structure-phylogeny repositions Avoralstat for SARS-CoV-2 prophylaxis in mice

doi: 10.1101/2021.01.04.425289

Figure Lengend Snippet: (a) HEK-cells treated with Camostat, Avoralstat, PCI-27483, Antipain, or SBTI 2-hr before TMPRSS2 transfection. TMPRSS2 reduced autoproteolysis (increased TMPRSS2-FL signal; *p<0.0332, **p<0.0021, ***p<0.0002). Calu-3-cells were treated with compounds and inoculated with pseudovirions harboring (b) VSV-G or (c) SARS-CoV-2-spike-protein. Calu-3 cells were treated with (d) 100 μM or (e) indicated concentrations of each compound, then incubated with SARS-CoV-2. Viral gRNA was measured after 24-hrs. Data represent mean ± SEM; n=3. (d) Compounds reduced viral signal at 100 μM (****p<0.0001). (e) Viral signal was reduced beginning from 100 nM (*p<0.0332, ****p<0.0001).

Article Snippet: Inhibition experiments were carried out in the presence of 50 μM Cbz-GGR-AMC in the presence 10 to 500 μM compound: Camostat (Sigma-Aldrich; Cat. # SML0057), Avoralstat (MedChemExpress; Cat. # HY-16735), PCI-27483 (Cayman Chemical; Item #21334), Antipain (Sigma-Aldrich; Product #A6191), Leupeptin (Sigma-Aldrich; Product #L2884), MDL-28170 (Sigma-Aldrich; Product #M6690), Ritonavir (Sigma-Aldrich; Product #SML0491), or 5% DMSO (as a negative control).

Techniques: Transfection, Incubation

(a-c) Ad5-hACE2-transduced BALB/c mice treated with Avoralstat, Camostat, or DMSO 4-hrs before and after SARS-CoV-2 viral challenge showed significantly reduced lung viral titer. (d) Avoralstat protected mice from weight-loss better than Camostat. (e) Avoralstat significantly reduced lung viral titer. (f) At the highest dose of SARS-CoV-2, Avoralstat protected mice from weight-loss. (f) Avoralstat and Camostat significantly lowered viral titer, n=6. (*p<0.0332, **p<0.0021, ***p<0.0002; mean ± SEM; L.O.D., limit of detection).

Journal: bioRxiv

Article Title: TMPRSS2 structure-phylogeny repositions Avoralstat for SARS-CoV-2 prophylaxis in mice

doi: 10.1101/2021.01.04.425289

Figure Lengend Snippet: (a-c) Ad5-hACE2-transduced BALB/c mice treated with Avoralstat, Camostat, or DMSO 4-hrs before and after SARS-CoV-2 viral challenge showed significantly reduced lung viral titer. (d) Avoralstat protected mice from weight-loss better than Camostat. (e) Avoralstat significantly reduced lung viral titer. (f) At the highest dose of SARS-CoV-2, Avoralstat protected mice from weight-loss. (f) Avoralstat and Camostat significantly lowered viral titer, n=6. (*p<0.0332, **p<0.0021, ***p<0.0002; mean ± SEM; L.O.D., limit of detection).

Article Snippet: Inhibition experiments were carried out in the presence of 50 μM Cbz-GGR-AMC in the presence 10 to 500 μM compound: Camostat (Sigma-Aldrich; Cat. # SML0057), Avoralstat (MedChemExpress; Cat. # HY-16735), PCI-27483 (Cayman Chemical; Item #21334), Antipain (Sigma-Aldrich; Product #A6191), Leupeptin (Sigma-Aldrich; Product #L2884), MDL-28170 (Sigma-Aldrich; Product #M6690), Ritonavir (Sigma-Aldrich; Product #SML0491), or 5% DMSO (as a negative control).

Techniques:

Treatments for C1-INH HAE under research.

Journal: Drugs in Context

Article Title: Breakthroughs in hereditary angioedema management: a systematic review of approved drugs and those under research

doi: 10.7573/dic.212605

Figure Lengend Snippet: Treatments for C1-INH HAE under research.

Article Snippet: Avoralstat ® , BioCryst Pharmaceuticals , Phase 3 trial for a long-term prophylaxis orally administered small kallikrein inhibitor..

Techniques: Virus, Plasmid Preparation, Expressing, Clinical Proteomics