HY-167353 Search Results


avoralstat  (MedChemExpress)
90
MedChemExpress avoralstat
(A) <t>Avoralstat</t> selectivity against 70 proteases. Top row — Cα-RMSD of pairwise structural alignments to TMPRSS2. (B) Protease inhibition by avoralstat correlates with 3DPhyloFold prediction. (C) TMPRSS2-S1P domain inhibition. IC50 data represent mean ± SEM; n = 3; calculated from the Hill equation.
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(A) Avoralstat selectivity against 70 proteases. Top row — Cα-RMSD of pairwise structural alignments to TMPRSS2. (B) Protease inhibition by avoralstat correlates with 3DPhyloFold prediction. (C) TMPRSS2-S1P domain inhibition. IC50 data represent mean ± SEM; n = 3; calculated from the Hill equation.

Journal: The Journal of Clinical Investigation

Article Title: Structure-based phylogeny identifies avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice

doi: 10.1172/JCI147973

Figure Lengend Snippet: (A) Avoralstat selectivity against 70 proteases. Top row — Cα-RMSD of pairwise structural alignments to TMPRSS2. (B) Protease inhibition by avoralstat correlates with 3DPhyloFold prediction. (C) TMPRSS2-S1P domain inhibition. IC50 data represent mean ± SEM; n = 3; calculated from the Hill equation.

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, SML0057), avoralstat (MedChemExpress, HY-16735), PCI-27483 (Cayman Chemical, 21334), antipain (Sigma-Aldrich, A6191), leupeptin (Sigma-Aldrich, L2884), MDL-28170 (Sigma-Aldrich, M6690), ritonavir (Sigma-Aldrich, SML0491), or 5% DMSO (as a negative control).

Techniques: Inhibition

(A and B) HEK cells treated with camostat, avoralstat, PCI-27483, antipain, or SBTI 2 hours before TMPRSS2 transfection. TMPRSS2 reduced autoproteolysis (increased TMPRSS2-FL signal; 1-way ANOVA followed by Dunnett’s multiple-comparison test; *P < 0.0332, **P < 0.0021, ***P < 0.0002 compared with vehicle; n = 5 for each group except vehicle and camostat [n =14]). Calu-3-cells were treated with compounds and inoculated with pseudovirions harboring (C) VSV-G or (D) SARS-CoV-2-spike-protein (n = 6; fit to the Hill equation). Calu-3 cells were treated with (E) 100 μM or (F) indicated concentrations of each compound, then incubated with SARS-CoV-2. Viral gRNA was measured after 24 hours. Data represent mean ± SEM; n = 3. (E) Compounds reduced viral signal at 100 μM (1-way ANOVA followed by Tukey’s multiple-comparison test; mean ± SEM; n = 3; ****P < 0.0001 compared with vehicle). (F) Viral signal was reduced beginning from 100 nM (2-way ANOVA followed by Dunnett’s multiple-comparison test; mean ± SEM; n = 3; *P < 0.0332, ****P < 0.0001 compared with vehicle).

Journal: The Journal of Clinical Investigation

Article Title: Structure-based phylogeny identifies avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice

doi: 10.1172/JCI147973

Figure Lengend Snippet: (A and B) HEK cells treated with camostat, avoralstat, PCI-27483, antipain, or SBTI 2 hours before TMPRSS2 transfection. TMPRSS2 reduced autoproteolysis (increased TMPRSS2-FL signal; 1-way ANOVA followed by Dunnett’s multiple-comparison test; *P < 0.0332, **P < 0.0021, ***P < 0.0002 compared with vehicle; n = 5 for each group except vehicle and camostat [n =14]). Calu-3-cells were treated with compounds and inoculated with pseudovirions harboring (C) VSV-G or (D) SARS-CoV-2-spike-protein (n = 6; fit to the Hill equation). Calu-3 cells were treated with (E) 100 μM or (F) indicated concentrations of each compound, then incubated with SARS-CoV-2. Viral gRNA was measured after 24 hours. Data represent mean ± SEM; n = 3. (E) Compounds reduced viral signal at 100 μM (1-way ANOVA followed by Tukey’s multiple-comparison test; mean ± SEM; n = 3; ****P < 0.0001 compared with vehicle). (F) Viral signal was reduced beginning from 100 nM (2-way ANOVA followed by Dunnett’s multiple-comparison test; mean ± SEM; n = 3; *P < 0.0332, ****P < 0.0001 compared with vehicle).

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, SML0057), avoralstat (MedChemExpress, HY-16735), PCI-27483 (Cayman Chemical, 21334), antipain (Sigma-Aldrich, A6191), leupeptin (Sigma-Aldrich, L2884), MDL-28170 (Sigma-Aldrich, M6690), ritonavir (Sigma-Aldrich, SML0491), or 5% DMSO (as a negative control).

Techniques: Transfection, Comparison, Incubation

(A–C) Ad5-hACE2-transduced BALB/c mice treated with avoralstat, camostat, or DMSO 4 hours before and after SARS-CoV-2 viral challenge showed significantly reduced lung viral titer (1-way ANOVA followed by Tukey’s multiple-comparison test; n = 3 or 4; LOD, limit of detection). (D) Avoralstat protected mice from weight loss better than camostat, n = 6 for each group (2-way ANOVA followed by Dunnett’s multiple-comparison test; *P < 0.0332, **P < 0.0021, ***P < 0.0002, ****P < 0.0001 compared with vehicle; mean ± SEM). (E) Avoralstat significantly reduced lung viral titer, n = 3 for each group (1-way ANOVA followed by Tukey’s multiple-comparison test). (F) At the highest dose of SARS-CoV-2, mouse weight loss was better mitigated by avoralstat compared with vehicle and camostat, n = 6 for each group (2-way ANOVA followed by Dunnett’s multiple-comparison test; *P < 0.0332, **P < 0.0021 compared with vehicle; mean ± SEM).

Journal: The Journal of Clinical Investigation

Article Title: Structure-based phylogeny identifies avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice

doi: 10.1172/JCI147973

Figure Lengend Snippet: (A–C) Ad5-hACE2-transduced BALB/c mice treated with avoralstat, camostat, or DMSO 4 hours before and after SARS-CoV-2 viral challenge showed significantly reduced lung viral titer (1-way ANOVA followed by Tukey’s multiple-comparison test; n = 3 or 4; LOD, limit of detection). (D) Avoralstat protected mice from weight loss better than camostat, n = 6 for each group (2-way ANOVA followed by Dunnett’s multiple-comparison test; *P < 0.0332, **P < 0.0021, ***P < 0.0002, ****P < 0.0001 compared with vehicle; mean ± SEM). (E) Avoralstat significantly reduced lung viral titer, n = 3 for each group (1-way ANOVA followed by Tukey’s multiple-comparison test). (F) At the highest dose of SARS-CoV-2, mouse weight loss was better mitigated by avoralstat compared with vehicle and camostat, n = 6 for each group (2-way ANOVA followed by Dunnett’s multiple-comparison test; *P < 0.0332, **P < 0.0021 compared with vehicle; mean ± SEM).

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, SML0057), avoralstat (MedChemExpress, HY-16735), PCI-27483 (Cayman Chemical, 21334), antipain (Sigma-Aldrich, A6191), leupeptin (Sigma-Aldrich, L2884), MDL-28170 (Sigma-Aldrich, M6690), ritonavir (Sigma-Aldrich, SML0491), or 5% DMSO (as a negative control).

Techniques: Comparison