Grazoprevir(MK-5172)
产品编号: DC9201
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应用领域
(1aR,5S,8S,10R,22aR)-5-tert-butyl-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxylic acid
| Cas No.: |
1206524-85-7 |
| 名称: |
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| 别名: |
MK 5172; MK5172 |
| SMILES: |
C1=CC2N=C3CCCCC[C@H]4C[C@@H]4OC(=O)N[C@H](C(C)(C)C)C(=O)N4[C@@H](C(N[C@@](C(=O)NS(C5CC5)(=O)=O)(C)[C@H](C)C=C)=O)C[C@@H](C4)OC3=NC=2C=C1OC |
| 分子式: |
C38H50N6O9S |
| 分子量: |
766.9 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| In Vivo: |
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| In Vitro: |
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| References: |
MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.
IC50 Value: 7.4 nM and 7 nM for genotype 1b and 1a respectively, in replicon system
Target: HCV NS3/4a protease
in vitro: In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a.
in vivo: In rats, MK-5172 showed a plasma clearance of 28 ml/min/kg and plasma half-life of 1.4 hr. When dosed p.o. at 5 mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7 uM.hr. The liver exposure of the compound was quite good (23 uM at 4 hr), and MK-5172 remained in liver 24 hr after a single p.o. 5 mg/kg dose. At 24 hr, the liver concentration of MK-5172 was 0.2 uM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5 ml/min/kg and a 3 hr half-life after i.v. 2 mg/kg dosing and had good plasma exposure (AUC=0.4 uM.hr) after a p.o. 1 mg/kg dose .
Clinical trial: Evaluation of Hepatic Pharmacokinetics for MK-5172 in Participants With Chronic Hepatitis C . Phase1. For the detailed information of MK-5172, the solubility of MK-5172 in water, the solubility of MK-5172 in DMSO, the solubility of MK-5172 in PBS buffer, the animal experiment (test) of MK-5172, the cell expriment (test) of MK-5172, the in vivo, in vitro and clinical trial test of MK-5172, the EC50, IC50,and affinity,of MK-5172, Please contact DC Chemicals. |
| Kinase Assay: |
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| Cell Assay: |
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| References: |
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MSDS
| TITLE |
DOWNLOAD |
| MSDS_2569_DC9201_1206524-85-7 |
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COA
| LOT NO. |
DOWNLOAD |
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