HCV Protease

HCV Protease抑制剂选择性比较

HCV Protease信号通路图

HCV Protease信号通路图

HCV Protease产品

  • 所有产品(24)
  • HCV Protease抑制剂 (24)
目录号 产品名 产品描述 文献引用 实验数据
S1482 Daclatasvir (BMS-790052) Daclatasvir (BMS-790052, EBP883) 是一种高度选择性的HCV NS5A抑制剂,EC50为9-50 pM,在细胞培养中,作用于多种HCV复制基因型和JFH-1基因型2a的感染性病毒。Phase 3。
Commun Biol, 2022, 5(1):154
Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5
bioRxiv, 2021, 2021.07.21.453274
S1538 Telaprevir (VX-950) Telaprevir (VX-950, LY-570310, MP-424)是一种丙型肝炎病毒(HCV)NS3-4A丝氨酸蛋白酶抑制剂,IC50为0.354 μM。
J Cell Biochem, 2022, 10.1002/jcb.30213
Cell Rep, 2021, 35(7):109133
Front Pharmacol, 2021, 12:773198
S1480 Lomibuvir (VX-222) Lomibuvir (VX-222, VCH-222)是一种新型的,有效的,选择性的HCV聚合酶抑制剂,IC50为0.94-1.2 μM,作用于突变型M423T效果低15.3倍,作用于突变型I482L效果低108倍。Phase 2。
J Virol, 2022, jvi0190621
Sci Rep, 2021, 11(1):19443
Antimicrob Agents Chemother, 2019, 63(6)
S1183 Danoprevir (ITMN-191) Danoprevir (ITMN-191, RG7227) 是一种肽类抑制剂,作用于丙型肝炎病毒(HCV)的NS3/4A蛋白酶IC50为0.2-3.5 nM,抑制HCV 1A/1B/4/5/6基因型比抑制2B/3A基因型效果高10倍左右。Phase 2。
J Cell Biochem, 2022, 10.1002/jcb.30213
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
S4935 Asunaprevir (BMS-650032) 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。
Cell Rep, 2021, 35(7):109133
bioRxiv, 2021, 10.1101/2021.07.16.452672
Viruses, 2021, 13(2)173
E0097New Mericitabine Mericitabine (RG 7128, R-7128, PSI 6130 diisobutyrate)是HCV NS5B聚合酶(HCV NS5B polymerase)的核苷抑制剂,作为RNA链终止子,在复制过程中防止RNA转录本的延伸。
S5404 Paritaprevir (ABT-450) Paritaprevir (ABT-450)是NS3/4A抑制剂。
Cell Rep, 2021, 35(7):109133
S5403 Ombitasvir (ABT-267) Ombitasvir (ABT-267)是HCV NS5A的抑制剂,具有抗病毒活性。
Commun Biol, 2022, 5(1):154
Sci Rep, 2021, 11(1):19443
bioRxiv, 2021, 2021.07.21.453274
S5402 Dasabuvir (ABT-333) Dasabuvir (ABT-333) is a non-nucleoside inhibitor of NS5B viral RNA-dependent RNA polymerase that inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates with IC50 values between 2.2 and 10.7 nM. It is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases.
Sci Rep, 2021, 11(1):19443
S3395 Tegobuvir Tegobuvir (TGV, GS 333126, GS-9190) 是一种 HCV RNA replication 的非核苷抑制剂,在被HCV感染的患者中已证明具有抗病毒的活性。
S9641 Pibrentasvir (ABT-530) Pibrentasvir (ABT-530) 是一种新型的泛基因型丙型肝炎病毒 hepatitis C virus (HCV) NS5A 抑制剂,其针对包含基因型1至6的NS5A的HCV复制子的EC50值为1.4 pM至5.0 pM。
S5720 Glecaprevir Glecaprevir is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that targets the the viral RNA replication. It displays IC50 values ranging from 3.5 to 11.3 nM for clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a.
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
S2794 Sofosbuvir (GS-7977) Sofosbuvir (PSI-7977, GS-7977) 是一种 HCV的NS5B polymerase抑制剂,用于治疗慢性丙型肝炎病毒(HCV)的感染。
Nat Commun, 2022, 13(1):2079
Front Oncol, 2021, 11:803278
Int J Mol Sci, 2021, 22(9)4559
S5394 Tizoxanide Tizoxanide (Desacetyl-nitazoxanide), a thiazolide anti-infective, is active against anaerobic bacteria, protozoa, and a range of viruses in cell culture models, and is currently in phase II clinical development for treating chronic hepatitis C.
S3728 Grazoprevir Grazoprevir anhydrous (MK5172) 是一种 Hepatitis C Virus NS3/4A Protease 的抑制剂,HCV genotype 1a、1B和4的IC50值分别为7pM、4pM和62pM。
Cell Rep, 2021, 35(7):109133
Front Oncol, 2021, 11:803278
Sci Rep, 2021, 11(1):19443
S5652 Elbasvir Elbasvir (MK8742) is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype.
S7579 Ledipasvir (GS5885) Ledipasvir (GS5885) 是一种HCV NS5A polymerase抑制剂,用于治疗丙型肝炎病毒感染。
Sci Rep, 2021, 11(1):19443
Cancers (Basel), 2019, 11(10)E1407
Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
S5062 Daclatasvir Dihydrochloride Daclatasvir是一种具有口服活性的抗病毒剂,抑制HCVNS5A区域,用于治疗慢性遗传型1和3类的HCV感染。
Commun Biol, 2022, 5(1):154
J Antimicrob Chemother, 2021, 76(7):1874-1885
Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5
S3800 Lycorine hydrochloride Lycorine (Galanthidine, Amarylline, Narcissine, Licorine), a natural alkaloid extracted from the Amaryllidaceae plant family, has been reported to exhibit a wide range of physiological effects, including the potential effect against cancer. It is an HCV inhibitor with strong activity.
Aging Cell, 2021, e13307
S3724 Velpatasvir Velpatasvir (GS-5816) 是二代NS5A抑制剂,抑制丙型肝炎病毒(HCV)的复制。
Front Oncol, 2021, 11:803278
Drug Metab Dispos, 2020, 48(12):1264-1270
Front Microbiol, 2020, 10:2936
S3733 Boceprevir Boceprevir (EBP 520, SCH 503034)是一种口服的、直接作用于hepatitis C virus (HCV) protease的抑制剂,对NS3蛋白酶的Ki值为14 nM。在治疗慢性肝炎C(genotype 1)中,常与其他抗病毒共同给药。
J Cell Biochem, 2022, 10.1002/jcb.30213
Cell Rep, 2021, 35(7):109133
Front Pharmacol, 2021, 12:773198
S2074 Mecarbinate Mecarbinate (Dimecarbin) 是Arbidol Hydrochloride的化学中间体。
S5307 PSI-6206 (GS-331007) PSI-6206 (RO-2433, GS-331007)是有效的HCV RNA依赖性RNA聚合酶抑制剂,靶向NS5B聚合酶
S5015 Simeprevir (TMC435) Simeprevir (TMC-435, TMC-435350) 一种竞争性的、可逆的、非共价结合的大环hepatitis C virus (HCV) NS3/4A protease抑制剂,直接抑制HCV病毒。它对HCV NS3/4A(genotypes 1a, 1b, 2, 4, 5, and 6)的平均IC50值小于13 nM,而对genotype 3的IC50值为37 nM。
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
Viruses, 2021, 13(2)173
S1482 Daclatasvir (BMS-790052) Daclatasvir (BMS-790052, EBP883) 是一种高度选择性的HCV NS5A抑制剂,EC50为9-50 pM,在细胞培养中,作用于多种HCV复制基因型和JFH-1基因型2a的感染性病毒。Phase 3。
Commun Biol, 2022, 5(1):154
Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5
bioRxiv, 2021, 2021.07.21.453274
S1538 Telaprevir (VX-950) Telaprevir (VX-950, LY-570310, MP-424)是一种丙型肝炎病毒(HCV)NS3-4A丝氨酸蛋白酶抑制剂,IC50为0.354 μM。
J Cell Biochem, 2022, 10.1002/jcb.30213
Cell Rep, 2021, 35(7):109133
Front Pharmacol, 2021, 12:773198
S1480 Lomibuvir (VX-222) Lomibuvir (VX-222, VCH-222)是一种新型的,有效的,选择性的HCV聚合酶抑制剂,IC50为0.94-1.2 μM,作用于突变型M423T效果低15.3倍,作用于突变型I482L效果低108倍。Phase 2。
J Virol, 2022, jvi0190621
Sci Rep, 2021, 11(1):19443
Antimicrob Agents Chemother, 2019, 63(6)
S1183 Danoprevir (ITMN-191) Danoprevir (ITMN-191, RG7227) 是一种肽类抑制剂,作用于丙型肝炎病毒(HCV)的NS3/4A蛋白酶IC50为0.2-3.5 nM,抑制HCV 1A/1B/4/5/6基因型比抑制2B/3A基因型效果高10倍左右。Phase 2。
J Cell Biochem, 2022, 10.1002/jcb.30213
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
S4935 Asunaprevir (BMS-650032) 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。
Cell Rep, 2021, 35(7):109133
bioRxiv, 2021, 10.1101/2021.07.16.452672
Viruses, 2021, 13(2)173
E0097New Mericitabine Mericitabine (RG 7128, R-7128, PSI 6130 diisobutyrate)是HCV NS5B聚合酶(HCV NS5B polymerase)的核苷抑制剂,作为RNA链终止子,在复制过程中防止RNA转录本的延伸。
S5404 Paritaprevir (ABT-450) Paritaprevir (ABT-450)是NS3/4A抑制剂。
Cell Rep, 2021, 35(7):109133
S5403 Ombitasvir (ABT-267) Ombitasvir (ABT-267)是HCV NS5A的抑制剂,具有抗病毒活性。
Commun Biol, 2022, 5(1):154
Sci Rep, 2021, 11(1):19443
bioRxiv, 2021, 2021.07.21.453274
S5402 Dasabuvir (ABT-333) Dasabuvir (ABT-333) is a non-nucleoside inhibitor of NS5B viral RNA-dependent RNA polymerase that inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates with IC50 values between 2.2 and 10.7 nM. It is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases.
Sci Rep, 2021, 11(1):19443
S3395 Tegobuvir Tegobuvir (TGV, GS 333126, GS-9190) 是一种 HCV RNA replication 的非核苷抑制剂,在被HCV感染的患者中已证明具有抗病毒的活性。
S9641 Pibrentasvir (ABT-530) Pibrentasvir (ABT-530) 是一种新型的泛基因型丙型肝炎病毒 hepatitis C virus (HCV) NS5A 抑制剂,其针对包含基因型1至6的NS5A的HCV复制子的EC50值为1.4 pM至5.0 pM。
S5720 Glecaprevir Glecaprevir is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that targets the the viral RNA replication. It displays IC50 values ranging from 3.5 to 11.3 nM for clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a.
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
S2794 Sofosbuvir (GS-7977) Sofosbuvir (PSI-7977, GS-7977) 是一种 HCV的NS5B polymerase抑制剂,用于治疗慢性丙型肝炎病毒(HCV)的感染。
Nat Commun, 2022, 13(1):2079
Front Oncol, 2021, 11:803278
Int J Mol Sci, 2021, 22(9)4559
S5394 Tizoxanide Tizoxanide (Desacetyl-nitazoxanide), a thiazolide anti-infective, is active against anaerobic bacteria, protozoa, and a range of viruses in cell culture models, and is currently in phase II clinical development for treating chronic hepatitis C.
S3728 Grazoprevir Grazoprevir anhydrous (MK5172) 是一种 Hepatitis C Virus NS3/4A Protease 的抑制剂,HCV genotype 1a、1B和4的IC50值分别为7pM、4pM和62pM。
Cell Rep, 2021, 35(7):109133
Front Oncol, 2021, 11:803278
Sci Rep, 2021, 11(1):19443
S5652 Elbasvir Elbasvir (MK8742) is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype.
S7579 Ledipasvir (GS5885) Ledipasvir (GS5885) 是一种HCV NS5A polymerase抑制剂,用于治疗丙型肝炎病毒感染。
Sci Rep, 2021, 11(1):19443
Cancers (Basel), 2019, 11(10)E1407
Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
S5062 Daclatasvir Dihydrochloride Daclatasvir是一种具有口服活性的抗病毒剂,抑制HCVNS5A区域,用于治疗慢性遗传型1和3类的HCV感染。
Commun Biol, 2022, 5(1):154
J Antimicrob Chemother, 2021, 76(7):1874-1885
Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5
S3800 Lycorine hydrochloride Lycorine (Galanthidine, Amarylline, Narcissine, Licorine), a natural alkaloid extracted from the Amaryllidaceae plant family, has been reported to exhibit a wide range of physiological effects, including the potential effect against cancer. It is an HCV inhibitor with strong activity.
Aging Cell, 2021, e13307
S3724 Velpatasvir Velpatasvir (GS-5816) 是二代NS5A抑制剂,抑制丙型肝炎病毒(HCV)的复制。
Front Oncol, 2021, 11:803278
Drug Metab Dispos, 2020, 48(12):1264-1270
Front Microbiol, 2020, 10:2936
S3733 Boceprevir Boceprevir (EBP 520, SCH 503034)是一种口服的、直接作用于hepatitis C virus (HCV) protease的抑制剂,对NS3蛋白酶的Ki值为14 nM。在治疗慢性肝炎C(genotype 1)中,常与其他抗病毒共同给药。
J Cell Biochem, 2022, 10.1002/jcb.30213
Cell Rep, 2021, 35(7):109133
Front Pharmacol, 2021, 12:773198
S2074 Mecarbinate Mecarbinate (Dimecarbin) 是Arbidol Hydrochloride的化学中间体。
S5307 PSI-6206 (GS-331007) PSI-6206 (RO-2433, GS-331007)是有效的HCV RNA依赖性RNA聚合酶抑制剂,靶向NS5B聚合酶
S5015 Simeprevir (TMC435) Simeprevir (TMC-435, TMC-435350) 一种竞争性的、可逆的、非共价结合的大环hepatitis C virus (HCV) NS3/4A protease抑制剂,直接抑制HCV病毒。它对HCV NS3/4A(genotypes 1a, 1b, 2, 4, 5, and 6)的平均IC50值小于13 nM,而对genotype 3的IC50值为37 nM。
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
Viruses, 2021, 13(2)173
E0097New Mericitabine Mericitabine (RG 7128, R-7128, PSI 6130 diisobutyrate)是HCV NS5B聚合酶(HCV NS5B polymerase)的核苷抑制剂,作为RNA链终止子,在复制过程中防止RNA转录本的延伸。
Tags: HCV protease treatment | HCV protease assay | HCV protease inhibitors review