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 3 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]
()
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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 NFfqbW9HfW6ldHnvckBie3OjeR?= NF;h[5ZKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKEiFVjDn[Y5wfHmyZTC0ZUBGTDR|IF7TN{Bxem:2ZXHz[UBqdiCpZX7veJlx\SBzYjDjc44yKHKncHzpZ49vKGOnbHzzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkCwNVfPxE1? MoPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NkS1N|IoRjJ5NU[0OVMzRC:jPh?=
Huh7.5 cells NUPZZ2ZsSW62aY\pdoFtKGG|c3H5 M1:5VWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEXiCpZX7veJlx\SBzYjDDc44yKGW6cILld5NqdmdiTmOzJJBzd3SnYYPlJIlv\mWldHXkJIlvKGi3bXHuJGh2cDdwNTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hfmm{YXygVm5CKHKncHzpZ4F1cW:wIHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjByM988US=> NUPWW4czRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OlQ2OzJpPkK3OVY1PTN{PD;hQi=>
HCV replicon cells M2TDXGFvfGm4aYLhcEBie3OjeR?= NUTCNYdUSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHhJGg4PyCrbjDIR3YhemWybHnjc44h[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwII\pdoFtKFKQQTDy[ZBtcWOjdHnvckBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6wNFTPxE1? M3zBNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NU[0OVMzLz5{N{W2OFU{OjxxYU6=
HCV replicon cells MUPBcpRqfmm{YXygZZN{[Xl? MmfSRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDKjIFrISk0yKGmwIFjDWkBz\XCuaXPvckBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5idnnyZYwhWk6DIILldIxq[2G2aX;uJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkKxO:69VQ>? MljYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NkS1N|IoRjJ5NU[0OVMzRC:jPh?=
genotype 2a replicon cells NITMNoJHfW6ldHnvckBie3OjeR?= MVfJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IH\1cIwhdGWwZ4ToJGhEXiCpZX7veJlx\SB{YjDIR{1LQCCQU{OgdJJwfGWjc3WgbY4h\2Wwb4T5dIUhOmFicnXwcIlkd25iY3XscJMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuOlIy|ryP NWH5NHhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OlQ2OzJpPkK3OVY1PTN{PD;hQi=>
genotype 2a replicon cells MV\GeY5kfGmxbjDhd5NigQ>? NIf0SHFKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKEiFVjDn[Y5wfHmyZTCzZUBUPTJiTmOzJJBzd3SnYYPlJIlvKGenbn;0fZBmKDKjIILldIxq[2:wIHPlcIx{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2xMlHPxE1? NHXaXW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W2OFU{Oid-Mke1OlQ2OzJ:L3G+
HuH7 cells MonURY51cX[rcnHsJIF{e2G7 M3y5NVMh\GG7cx?= NV3xOXV6SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHiJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[XRiPk2gNVAhfGmvZYOgZY51cX[rcnHsJGVEPTBiYX\0[ZIhOyCmYYnzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiYYPzZZk> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR|MESzO{c,Ojh2M{C0N|c9N2F-
HuH7 cells NWfHV2FQSW62aY\pdoFtKGG|c3H5 M2PCR|Mh\GG7cx?= M1qxbGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEXiCpZX7veJlx\SBzYjDpcoZm[3SnZDDpckBpfW2jbjDIeWg4KGOnbHzzJINwNXS{ZXH0[YQhf2m2aDDkZYNt[XSjc4\pdkBi\nSncjCzJIRigXNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeR?= NWWzTWh1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|A1OzdpPkK4OFMxPDN5PD;hQi=>
HuH7 replicon cells NWrQeJRQTnWwY4Tpc44h[XO|YYm= MYm0JIRigXN? MkGzTY5pcWKrdHnvckBw\iCKQ2[g[4Vvd3S7cHWgNYIhS2:wMTDOV|MheHKxdHXhd4UhcW6oZXP0[YQhcW5iaIXtZY4hUHWKNzDy[ZBtcWOxbjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hfmm{YXygdoVxdGmlYYTpc44h[W[2ZYKgOEBl[Xm|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjByMUNOwG0> M1r6fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MU[yOFU1Lz5{OUG2NlQ2PDxxYU6=
HuH7 replicon cells MVnGeY5kfGmxbjDhd5NigQ>? NVjm[HVGPCCmYYnz MoDVTY5pcWKrdHnvckBw\iCKQ2[g[4Vvd3S7cHWgNYEhUDd5IF7TN{Bxem:2ZXHz[UBqdm[nY4Tl[EBqdiCqdX3hckBJfUh5IILldIxq[2:wIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjC0JIRigXNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvODB2zszN M1jMTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MU[yOFU1Lz5{OUG2NlQ2PDxxYU6=
HuH7.5 cells M3nnV2FvfGm4aYLhcEBie3OjeR?= NF24cGo1KGSjeYO= M1izbWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEXiCpZX7veJlx\SBzYjDDc44yKGmwZnXjeIVlKGmwIHj1cYFvKEi3SEeuOUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wIHHmeIVzKDRiZHH5d{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6wNFbPxE1? M3nCT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEW2PFA{Lz5{OUS1OlgxOzxxYU6=
Huh7.5 replicon cells NXTsb|JuSW62aY\pdoFtKGG|c3H5 NGLKOW01KGSjeYO= Mn;YRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1bFcvPSC{ZYDsbYNwdiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6geolz[WxicnXwcIlk[XSrb36gbY5kfWKjdHXkJIZweiB2IHThfZMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuNFA3|ryP Mn3DQIEhfGG{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:

    --

  • (Only for Reference)
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
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(133.63 mM)
Water Insoluble
Ethanol ''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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 Unknown status 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 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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