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MedChemexpress LLC
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Product Name:MK-5172 (sodium salt)
CAS:1425038-27-2
Purity:>98% Package:800RMB/1mg
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| Company Name: |
LETOPHARM LIMITED
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+86-21-5821 5861 |
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sales@letopharm.com |
| Products Intro: |
Product Name:MK-5172 (sodiuM salt)
CAS:1425038-27-2
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| | MK 5172 sodiuM salt Basic information |
| Product Name: | MK 5172 sodiuM salt | | Synonyms: | MK 5172 sodiuM salt;MK-5172 (sodiuM salt);MK5172 sodiuM salt;MK-5172 Sodium;Grazoprevir sodium salt;GRAZOPREVIR SODIUM SALT;MK5172 SODIUM SALT;MK 5172 SODIUM SALT | | CAS: | 1425038-27-2 | | MF: | C38H50N6NaO9S+ | | MW: | 790.91 | | EINECS: | | | Product Categories: | | | Mol File: | 1425038-27-2.mol |  |
| | MK 5172 sodiuM salt Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Powder |
| | MK 5172 sodiuM salt Usage And Synthesis |
| Description | 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 [1]
Target: HCV NS3/4a protease | | in vitro | 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 [2]. | | in vivo | 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 [1].
Clinical trial: Evaluation of Hepatic Pharmacokinetics for MK-5172 in Participants With Chronic Hepatitis C . Phase1 | | References | References:[1]. Steven Harper , John A. McCauley , Michael T. Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor. ACS Med. Chem. Lett., 2012, 3 (4), pp 332-336
[2]. Summa V, Ludmerer SW, McCauley JA, MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants. Antimicrob Agents Chemother. 2012 Aug;56(8):4161-7. |
| | MK 5172 sodiuM salt Preparation Products And Raw materials |
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