Asunaprevir (BMS-650032)

Catalog No.S4935

For research use only.

Asunaprevir (BMS-650032) is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.

Asunaprevir (BMS-650032) Chemical Structure

CAS No. 630420-16-5

Selleck's Asunaprevir (BMS-650032) has been cited by 4 Publications

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Biological Activity

Description Asunaprevir (BMS-650032) is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.
Targets
1b (J4L6S) [1] 1a (H77) [1] 6a (HK-6A) [1] 4a (ED43) [1] 5a (SA13) [1] Click to View More Targets
0.3 nM 0.7 nM 0.9 nM 1.6 nM 1.7 nM
In vitro

Asunaprevir (ASV) competitively binds to the NS3/4A protease complex, with Ki values of 0.4 and 0.24 nM against recombinant enzymes representing genotypes 1a (H77) and 1b (J4L6S), respectively. Asunaprevir is high selective without any significant activity against the closely related GB virus-B NS3 protease and a panel of human serine or cysteine proteases. In cell culture, ASV inhibits replication of HCV replicons representing genotypes 1 and 4, with 50% effective concentrations (EC50s) ranging from 1 to 4 nM, and has weaker activity against genotypes 2 and 3 (EC50, 67-1162 nM). Selectivity is again demonstrated by the absence of activity (EC50, >12 μM) against a panel of other RNA viruses[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
genotype 1b con1 replicon cells MlfiSpVv[3Srb36gZZN{[Xl? NGjhVHVKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKEiFVjDn[Y5wfHmyZTC0ZUBGTDR|IF7TN{Bxem:2ZXHz[UBqdiCpZX7veJlx\SBzYjDjc44yKHKncHzpZ49vKGOnbHzzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkCwNVfPxE1? M2rhOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NU[0OVMzLz5{N{W2OFU{OjxxYU6=
Huh7.5 cells M3ruSWFvfGm4aYLhcEBie3OjeR?= MV\BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhOWJiQ3;uNUBmgHC{ZYPzbY5oKE6VMzDwdo91\WG|ZTDpcoZm[3SnZDDpckBpfW2jbjDIeYg4NjViY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJJZqemGuIGLORUBz\XCuaXPheIlwdiCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NE4xODQQvF2= M1OzSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NU[0OVMzLz5{N{W2OFU{OjxxYU6=
HCV replicon cells MmnWRY51cX[rcnHsJIF{e2G7 MoLjRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGjIFi3O{BqdiCKQ2[gdoVxdGmlb36gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKH[rcnHsJHJPSSC{ZYDsbYNifGmxbjDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5yMEVOwG0> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV4NEWzNkc,Ojd3NkS1N|I9N2F-
HCV replicon cells MWDBcpRqfmm{YXygZZN{[Xl? NGq5UZFCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJS1ZiZ3Xuc5R6eGViMnGgTmhHNTFiaX6gTGNXKHKncHzpZ49vKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjD2bZJidCCUTlGgdoVxdGmlYYTpc44h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuNlE4|ryP MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV4NEWzNkc,Ojd3NkS1N|I9N2F-
genotype 2a replicon cells NHrJcYxHfW6ldHnvckBie3OjeR?= MofhTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDmeYxtKGynbnf0bEBJS1ZiZ3Xuc5R6eGViMnKgTGMuUjhiTmOzJJBzd3SnYYPlJIlvKGenbn;0fZBmKDKjIILldIxq[2:wIHPlcIx{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlYzOc7:TR?= M4PN[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NU[0OVMzLz5{N{W2OFU{OjxxYU6=
genotype 2a replicon cells MknLSpVv[3Srb36gZZN{[Xl? NGHpeXFKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKEiFVjDn[Y5wfHmyZTCzZUBUPTJiTmOzJJBzd3SnYYPlJIlvKGenbn;0fZBmKDKjIILldIxq[2:wIHPlcIx{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2xMlHPxE1? MlHoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NkS1N|IoRjJ5NU[0OVMzRC:jPh?=
HuH7 cells NIru[G1CdnSrdnnyZYwh[XO|YYm= NXTHUWlvOyCmYYnz MlfpRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1TFch[2WubIOgZZQhRj1iMUCgeIlu\XNiYX70bZZqemGuIFXDOVAh[W[2ZYKgN{Bl[Xm|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYm= NFrCRlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNFQ{Pyd-Mki0N|A1Ozd:L3G+
HuH7 cells NIrQeJhCdnSrdnnyZYwh[XO|YYm= NInqTnA{KGSjeYO= MX;BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDjc{11emWjdHXkJJdqfGhiZHHjcIF1[XO4aYKgZYZ1\XJiMzDkZZl{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{[Xl? NG\uTnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNFQ{Pyd-Mki0N|A1Ozd:L3G+
HuH7 replicon cells MmroSpVv[3Srb36gZZN{[Xl? MmPROEBl[Xm| NGW5XY1KdmirYnn0bY9vKG:oIFjDWkBo\W6xdInw[UAy[iCFb36xJG5UOyCycn;0[YF{\SCrbn\lZ5Rm\CCrbjDoeY1idiCKdVi3JJJmeGyrY3;uJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC4aYLhcEBz\XCuaXPheIlwdiCjZoTldkA1KGSjeYOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMECxNu69VQ>? M3Pm[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MU[yOFU1Lz5{OUG2NlQ2PDxxYU6=
HuH7 replicon cells MYnGeY5kfGmxbjDhd5NigQ>? M2TIXFQh\GG7cx?= NFjEbpZKdmirYnn0bY9vKG:oIFjDWkBo\W6xdInw[UAy[SCKN{egUnM{KHC{b4TlZZNmKGmwZnXjeIVlKGmwIHj1cYFvKEi3SEegdoVxdGmlb36gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKH[rcnHsJJJmeGyrY3H0bY9vKGGodHXyJFQh\GG7czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5yMEVOwG0> NYrzTVFtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOlI1PTRpPkK5NVYzPDV2PD;hQi=>
HuH7.5 cells MkK4RY51cX[rcnHsJIF{e2G7 NFTacW81KGSjeYO= NIrDeXpCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJS1ZiZ3Xuc5R6eGViMXKgR49vOSCrbn\lZ5Rm\CCrbjDoeY1idiCKdVi3MlUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCC{ZYDsbYNifGmxbjDh[pRmeiB2IHThfZMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuNFA3|ryP MoLMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NU[4NFMoRjJ7NEW2PFA{RC:jPh?=
Huh7.5 replicon cells NV7ze|Z1SW62aY\pdoFtKGG|c3H5 NVW4cXlRPCCmYYnz NWnjbm5kSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHiJIlv\mWldHXkJIlvKGi3bXHuJGh2cDdwNTDy[ZBtcWOxbjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hfmm{YXygdoVxdGmlYYTpc44hcW6ldXLheIVlKG[xcjC0JIRigXNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvODB4zszN Mnj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NUCyPVAoRjJ7NkWwNlkxRC:jPh?=
In vivo Plasma and tissue exposures in vivo in several animal species indicate that ASV displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species). Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50s observed with HCV genotype-1 replicons[1].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: Huh 7.5.1 cells
  • Concentrations: 1 or 10 nM
  • Incubation Time: 3, 6, 24, and 48 h
  • Method:

    --

Animal Research:

[1]

  • Animal Models: male FVB mice, Sprague-Dawley rats, male beagles, male cynomolgus monkeys
  • Dosages: 5 mg/kg (mice); 3, 5, 10, and 15 mg/kg (rats); 3 or 6 mg/kg (Dogs); 3 mg/kg (Monkeys)
  • Administration: by oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 748.29
Formula

C35H46ClN5O9S

CAS No. 630420-16-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C)C(C(=O)N1CC(CC1C(=O)NC2(CC2C=C)C(=O)NS(=O)(=O)C3CC3)OC4=NC=C(C5=C4C=C(C=C5)Cl)OC)NC(=O)OC(C)(C)C

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03208322 Withdrawn Other: Non-Interventional Hepatitis C Bristol-Myers Squibb November 30 2018 --
NCT03004625 Completed Drug: daclatasvir|Drug: asunaprevir|Drug: Ribavirin Hepatitis C Kaohsiung Medical University Chung-Ho Memorial Hospital|Chang Gung Memorial Hospital|National Taiwan University Hospital|Taipei Veterans General Hospital Taiwan|China Medical University Hospital|National Cheng-Kung University Hospital November 2016 Phase 3
NCT02865369 Not yet recruiting Drug: Daclatasvir and Asunaprevir Chronic Hepatitis C Sang Gyune Kim|Seoul National University Boramae Hospital|Severance Hospital|Inha University Hospital|Korea University|Gachon University Gil Medical Center|Hanyang University Seoul Hospital|Ewha Womans University Mokdong Hospital|Bristol-Myers Squibb|Soonchunhyang University Hospital September 2016 --
NCT02580474 Completed Drug: Daclatasvir plus Asunaprevir Hepatitis C Myeong Jun Song|Bristol-Myers Squibb|Soonchunhyang University Hospital|Dankook University|Chungnam National University Hospital|Konyang University Hospital|Eulji University Hospital|Saint Vincent''s Hospital Korea|Konkuk University Hospital|Cheongju St. Mary''s Hospital Cheongju Korea|Severance Hospital|Korea University Guro Hospital|Eulji General Hospital|The Catholic University of Korea February 2016 Phase 4
NCT02496078 Completed Drug: Daclatasvir|Drug: Asunaprevir Hepatitis C Bristol-Myers Squibb August 2015 Phase 3
NCT02309450 Withdrawn Drug: .Asunaprevir Daclatasvir and BMS - 791325 Hepatitis C Virus Genotype 4 Infection ANRS Emerging Infectious Diseases|Bristol-Myers Squibb December 2014 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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