HCV Protease
信号通路图
研究领域
抑制剂选择性比较
HCV Protease产品
| 目录号 | 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。 |
The toxicity of BMS-790052 (BMS) and Telaprevir (TPV) was measured by seeding 96-well plates to 70% confluence and exposing the cells to up to 50 μM of compound for 72 hours. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] was added to each well at a final concentration of 500 μg/ml 4 h before dissolving crystals in 100 μl of DMSO and measuring at 550 nm UV wavelengths. The 50% cytotoxic concentration (CC50) was then calculation using the OD550 value and the following formula: log CC50=log concentration of HPP-[(HPP-50)/(HPP-LPP)×log d HPP: highest protective percentage closest to 50% LPP: Lowest protective percentage closest to 50% d: dilution factor |
|
| 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。 |
HCV replicon genotype 1b cells were passaged in the presence of G418 alone (medium 694 control) or G418 with miravirsen, SPC4729 (oligonucleotide negative control) or telaprevir for 28 days in fixed concentrations at a multiple (X) of the EC50 of miravirsen or telaprevir. Colony formation was assessed by staining surviving cells with crystal violet.
|
|
| 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。 |
Genetic barriers of JTK-853, NNI-A, PF-868554, VX-222, PSI-6130, BMS-790052, and TMC435 for Con1. VX-222 and the other DAAs were treated at 1/3xEC90 for 17 days. |
|
| 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。 |
Western blot analysis of HCV NS3 protease cleavage of MAVS. The catalytic efficiency of four proteases (H, H-A156T, 41 and 41-A156T) from individuals H and 41 were tested in the absence or presence of an NS3 protease inhibitor (danoprevir). Expression of the HCV NS3 proteases resulted in cleavage of the lambda cI repressor with MAVS cleavage site. Expression of the protease was induced with IPTG for 3 h. The lambda cI repressor with MAVS cleavage site was not cleaved by an NS3 protease that included a substitution in catalytic residue S139A. Similarly, different catalytic efficiencies were observed with different proteases.
|
|
| 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。 |
||
| S5404 |
Paritaprevir (ABT-450)Paritaprevir (ABT-450)是NS3/4A抑制剂。 |
||
| S5403 |
Ombitasvir (ABT-267)Ombitasvir (ABT-267)是HCV NS5A的抑制剂，具有抗病毒活性。 |
||
| 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. |
||
| S3395 |
TegobuvirTegobuvir (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 |
GlecaprevirGlecaprevir 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. |
||
| 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。 |
Representative confocal microscope image showing phosphorylated Drp1 translocation to mitochondria and mitochondrial fission in the presence of Sofosbuvir. At 24 hours after treatment with Sofosbuvir (100 nM), Huh7 cells were immunostained with antibodies against TOM20 (red) and p-Drp1 (S616) (green). Nuclei are demarcated with white dotted circles. Treated (+) and untreated (–) cells are marked. In the zoomed images, the arrows indicate the colocalization of TOM20 and p-Drp1 (S616) in Sofosbuvir-treated cells (yellow spots).
|
|
| S5394 |
TizoxanideTizoxanide (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 |
GrazoprevirGrazoprevir 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。 |
||
| S5652 |
ElbasvirElbasvir (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。 |
(C) Impact of HCV clearance by DAA treatment on the Nrf2 nuclear translocation. HCV infected Huh-7.5 cells day 12 were given two rounds of antiviral treatment with IFN-α, sofosbuvir, ledipasvir or combination of sofosbuvir plus ledipasvir. After 72 hours, cells were split, and then treated again with the same antiviral agent. After two rounds of antiviral treatment, the expressions of HCV core and pNrf2 were measured by immunostaining.
|
|
| S5062 |
Daclatasvir DihydrochlorideDaclatasvir是一种具有口服活性的抗病毒剂，抑制HCV的NS5A区域，用于治疗慢性遗传型1和3类的HCV感染。 |
||
| S3800 |
Lycorine hydrochlorideLycorine (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. |
||
| S3724 |
VelpatasvirVelpatasvir (GS-5816) 是二代NS5A抑制剂，抑制丙型肝炎病毒（HCV）的复制。 |
||
| S3733 |
BoceprevirBoceprevir (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。 |
||
| S2074 |
MecarbinateMecarbinate (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。 |
| 目录号 | 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。 |
The toxicity of BMS-790052 (BMS) and Telaprevir (TPV) was measured by seeding 96-well plates to 70% confluence and exposing the cells to up to 50 μM of compound for 72 hours. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] was added to each well at a final concentration of 500 μg/ml 4 h before dissolving crystals in 100 μl of DMSO and measuring at 550 nm UV wavelengths. The 50% cytotoxic concentration (CC50) was then calculation using the OD550 value and the following formula: log CC50=log concentration of HPP-[(HPP-50)/(HPP-LPP)×log d HPP: highest protective percentage closest to 50% LPP: Lowest protective percentage closest to 50% d: dilution factor |
|
| 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。 |
HCV replicon genotype 1b cells were passaged in the presence of G418 alone (medium 694 control) or G418 with miravirsen, SPC4729 (oligonucleotide negative control) or telaprevir for 28 days in fixed concentrations at a multiple (X) of the EC50 of miravirsen or telaprevir. Colony formation was assessed by staining surviving cells with crystal violet.
|
|
| 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。 |
Genetic barriers of JTK-853, NNI-A, PF-868554, VX-222, PSI-6130, BMS-790052, and TMC435 for Con1. VX-222 and the other DAAs were treated at 1/3xEC90 for 17 days. |
|
| 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。 |
Western blot analysis of HCV NS3 protease cleavage of MAVS. The catalytic efficiency of four proteases (H, H-A156T, 41 and 41-A156T) from individuals H and 41 were tested in the absence or presence of an NS3 protease inhibitor (danoprevir). Expression of the HCV NS3 proteases resulted in cleavage of the lambda cI repressor with MAVS cleavage site. Expression of the protease was induced with IPTG for 3 h. The lambda cI repressor with MAVS cleavage site was not cleaved by an NS3 protease that included a substitution in catalytic residue S139A. Similarly, different catalytic efficiencies were observed with different proteases.
|
|
| 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。 |
||
| S5404 |
Paritaprevir (ABT-450)Paritaprevir (ABT-450)是NS3/4A抑制剂。 |
||
| S5403 |
Ombitasvir (ABT-267)Ombitasvir (ABT-267)是HCV NS5A的抑制剂，具有抗病毒活性。 |
||
| 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. |
||
| S3395 |
TegobuvirTegobuvir (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 |
GlecaprevirGlecaprevir 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. |
||
| 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。 |
Representative confocal microscope image showing phosphorylated Drp1 translocation to mitochondria and mitochondrial fission in the presence of Sofosbuvir. At 24 hours after treatment with Sofosbuvir (100 nM), Huh7 cells were immunostained with antibodies against TOM20 (red) and p-Drp1 (S616) (green). Nuclei are demarcated with white dotted circles. Treated (+) and untreated (–) cells are marked. In the zoomed images, the arrows indicate the colocalization of TOM20 and p-Drp1 (S616) in Sofosbuvir-treated cells (yellow spots).
|
|
| S5394 |
TizoxanideTizoxanide (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 |
GrazoprevirGrazoprevir 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。 |
||
| S5652 |
ElbasvirElbasvir (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。 |
(C) Impact of HCV clearance by DAA treatment on the Nrf2 nuclear translocation. HCV infected Huh-7.5 cells day 12 were given two rounds of antiviral treatment with IFN-α, sofosbuvir, ledipasvir or combination of sofosbuvir plus ledipasvir. After 72 hours, cells were split, and then treated again with the same antiviral agent. After two rounds of antiviral treatment, the expressions of HCV core and pNrf2 were measured by immunostaining.
|
|
| S5062 |
Daclatasvir DihydrochlorideDaclatasvir是一种具有口服活性的抗病毒剂，抑制HCV的NS5A区域，用于治疗慢性遗传型1和3类的HCV感染。 |
||
| S3800 |
Lycorine hydrochlorideLycorine (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. |
||
| S3724 |
VelpatasvirVelpatasvir (GS-5816) 是二代NS5A抑制剂，抑制丙型肝炎病毒（HCV）的复制。 |
||
| S3733 |
BoceprevirBoceprevir (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。 |
||
| S2074 |
MecarbinateMecarbinate (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。 |
沪公网安备 31011502012800号