TELAPREVIR
Cyclopenta(c)pyrrole-1-carboxamide, (2S)-2-cyclohexyl-N-(pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-((1S)-1-((cyclopropylamino)oxoacetyl)butyl)octahydro-, (1S,3aR,6aS)-
CAS: 402957-28-2
Molecular Formula: C36H53N7O6
TELAPREVIR - Names and Identifiers
TELAPREVIR - Physico-chemical Properties
| Molecular Formula | C36H53N7O6 |
| Molar Mass | 679.85 |
| Density | 1.25 |
| Melting Point | 116-123°C |
| Solubility | ≥136 mg/mL in DMSO <1 mg/mL in Water <1 mg/mL in Ethanol |
| Appearance | Solid |
| Color | Pale Yellow to Light Yellow Waxy to |
| pKa | 11.84±0.20(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Use | Treatment of hepatitis C Virus (HCV) infection |
| In vitro study | Telaprevir acts on Con1 (genotype 1b) subgenomic HCV replicating cells and inhibits the serine protease NS3-4A hepatitis C virus, resulting in inhibition of viral polyprotein processing and subsequent replication of viral RNA, all HCV RNA and protein levels were reduced in a time-and dose-dependent manner. Telaprevir significantly promoted the inhibition of HCV RNA replication. After incubation for 24, 48, 72 and 120 hours, the IC50 values were 0.574 μ M and 0.488 μ M respectively, 0.210 μm and 0.139 μm, this effect is time-dependent. Telaprevir treatment of HCV replicating cells, parental Huh-7 and HepG2 cells for 48 hours showed no toxicity to the cells. 17.5 μm Telaprevir completely eliminated HCV RNA in replicating cells, and there was no rebound after 13 days of withdrawal treatment. The combination of Telaprevir and IFN-α, compared with the two agents alone, modestly improved synergy, reduced HCV RNA replication, and inhibited drug-resistant mutations, but had no apparent toxicity. |
| In vivo study | Telaprevir at doses of 10 and 25 mg/kg, treated orally in a mouse model, reduced HCV Protease-dependent cleavage and SEAP secretion from the liver into the blood by 18.7 and 18.4, respectively. Treatment of mice with genotype 1b HCV infected with human hepatocytes with Telaprevir at a dose of 200 mg/kg for 1 week resulted in a decrease in HCV RNA, and treatment of mice with MK-0608 (50 mg/kg), continued for 4 weeks, can completely remove the virus in mice. |
TELAPREVIR - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| HS Code | 29339900 |
TELAPREVIR - Introduction
Telaprevir (VX-950) is a serine protease inhibitor NS3-4A by hepatitis C virus (HCV) with an IC50 of 0.354 μM.
Last Update：2022-10-16 17:25:06
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Product Name: Telaprevir Visit Supplier Webpage Request for quotationCAS: 402957-28-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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