Asunaprevir (BMS-650032)

For research use only. Not for use in humans.

目录号:S4935 中文名称:阿那匹韦

Asunaprevir (BMS-650032) Chemical Structure

CAS No. 630420-16-5

Asunaprevir (BMS-650032)是具有口服活性的HCV NS3抑制剂。HCV NS3是病毒复制蛋白加工所必需的蛋白酶。

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客户使用Selleck生产的Asunaprevir (BMS-650032)发表文献3篇:

产品安全说明书

HCV Protease抑制剂选择性比较

生物活性

产品描述 Asunaprevir (BMS-650032)是具有口服活性的HCV NS3抑制剂。HCV NS3是病毒复制蛋白加工所必需的蛋白酶。
靶点
1b (J4L6S) [1]
()
1a (H77) [1]
()
6a (HK-6A) [1]
()
4a (ED43) [1]
()
5a (SA13) [1]
()
0.3 nM 0.7 nM 0.9 nM 1.6 nM 1.7 nM
体外研究

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 NWXnfXpqTnWwY4Tpc44h[XO|YYm= MoTSTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDmeYxtKGynbnf0bEBJS1ZiZ3Xuc5R6eGViNHGgSWQ1OyCQU{OgdJJwfGWjc3WgbY4h\2Wwb4T5dIUhOWJiY3;uNUBz\XCuaXPvckBk\WyuczDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5yMEG3{txO MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV4NEWzNkc,Ojd3NkS1N|I9N2F-
Huh7.5 cells NFTUcYVCdnSrdnnyZYwh[XO|YYm= NVfLZmozSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHiJGNwdjFiZYjwdoV{e2mwZzDOV|MheHKxdHXhd4UhcW6oZXP0[YQhcW5iaIXtZY4hUHWqNz61JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC4aYLhcEBTVkFicnXwcIlk[XSrb36gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMECz{txO M3rsdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NU[0OVMzLz5{N{W2OFU{OjxxYU6=
HCV replicon cells NFTZT3BCdnSrdnnyZYwh[XO|YYm= M4L0UWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEXiCpZX7veJlx\SBzYTDIO|chcW5iSFPWJJJmeGyrY3;uJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC4aYLhcEBTVkFicnXwcIlk[XSrb36gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMEC0{txO MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV4NEWzNkc,Ojd3NkS1N|I9N2F-
HCV replicon cells MX7BcpRqfmm{YXygZZN{[Xl? M4q3XmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEXiCpZX7veJlx\SB{YTDKTGYuOSCrbjDIR3YhemWybHnjc44h[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwII\pdoFtKFKQQTDy[ZBtcWOjdHnvckBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6yNVfPxE1? M4OzblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NU[0OVMzLz5{N{W2OFU{OjxxYU6=
genotype 2a replicon cells NF3YWHFHfW6ldHnvckBie3OjeR?= NX6yd|lDUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBnfWyuIHzlcod1cCCKQ2[g[4Vvd3S7cHWgNoIhUENvSkigUnM{KHC{b4TlZZNmKGmwIHflco91gXCnIELhJJJmeGyrY3;uJINmdGy|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjZ{Md88US=> NIflbFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W2OFU{Oid-Mke1OlQ2OzJ:L3G+
genotype 2a replicon cells MX3GeY5kfGmxbjDhd5NigQ>? NF\aXolKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKEiFVjDn[Y5wfHmyZTCzZUBUPTJiTmOzJJBzd3SnYYPlJIlvKGenbn;0fZBmKDKjIILldIxq[2:wIHPlcIx{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2xMlHPxE1? NETFW289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W2OFU{Oid-Mke1OlQ2OzJ:L3G+
HuH7 cells MXfBcpRqfmm{YXygZZN{[Xl? NUS3NWgxOyCmYYnz MXrBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDheEA,RSBzMDD0bY1meyCjboTpeolz[WxiRVO1NEBi\nSncjCzJIRigXNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeR?= NW\EUlZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|A1OzdpPkK4OFMxPDN5PD;hQi=>
HuH7 cells NGjoWHZCdnSrdnnyZYwh[XO|YYm= MnfqN{Bl[Xm| MnTGRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1TFch[2WubIOgZ48ufHKnYYTl[EB4cXSqIHThZ4xifGG|dnnyJIFnfGW{IEOg[IF6eyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7 NXfTPIttRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|A1OzdpPkK4OFMxPDN5PD;hQi=>
HuH7 replicon cells MVrGeY5kfGmxbjDhd5NigQ>? NWTHO5R4PCCmYYnz NH;HOmJKdmirYnn0bY9vKG:oIFjDWkBo\W6xdInw[UAy[iCFb36xJG5UOyCycn;0[YF{\SCrbn\lZ5Rm\CCrbjDoeY1idiCKdVi3JJJmeGyrY3;uJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC4aYLhcEBz\XCuaXPheIlwdiCjZoTldkA1KGSjeYOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMECxNu69VQ>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF4MkS1OEc,OjlzNkK0OVQ9N2F-
HuH7 replicon cells MkDqSpVv[3Srb36gZZN{[Xl? NVr5RYFjPCCmYYnz NUjGclJ1UW6qaXLpeIlwdiCxZjDIR3Yh\2Wwb4T5dIUhOWFiSEe3JG5UOyCycn;0[YF{\SCrbn\lZ5Rm\CCrbjDoeY1idiCKdVi3JJJmeGyrY3;uJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC4aYLhcEBz\XCuaXPheIlwdiCjZoTldkA1KGSjeYOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMEC0{txO NYjnd3BVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOlI1PTRpPkK5NVYzPDV2PD;hQi=>
HuH7.5 cells M{D3dmFvfGm4aYLhcEBie3OjeR?= NIPISWw1KGSjeYO= MlX6RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIFPvclEhcW6oZXP0[YQhcW5iaIXtZY4hUHWKNz61JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25iYX\0[ZIhPCCmYYnzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkCwOu69VQ>? NVLWSWE2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVY5ODNpPkK5OFU3QDB|PD;hQi=>
Huh7.5 replicon cells MkjrRY51cX[rcnHsJIF{e2G7 M{jSUVQh\GG7cx?= MUfBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXoO{42KHKncHzpZ49vKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjD2bZJidCC{ZYDsbYNifGmxbjDpcoN2[mG2ZXSg[o9zKDRiZHH5d{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6wNFbPxE1? NInMZ4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[1NFI6OCd-Mkm2OVAzQTB:L3G+

... Click to View More Cell Line Experimental Data

体内研究 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].

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[2]

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

    --


    (Only for Reference)
动物实验:

[1]

- 合并
  • 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)

溶解度 (25°C)

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

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 748.29
化学式

C35H46ClN5O9S

CAS号 630420-16-5
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID