MK 5172 potassiuM salt
- Product Name
- MK 5172 potassiuM salt
- CAS No.
- 1206524-86-8
- Chemical Name
- MK 5172 potassiuM salt
- Synonyms
- MK-5172 Potassium;Grazoprevir potassium;MK5172 potassiuM salt;MK 5172 potassiuM salt;MK-5172 (potassiuM salt);Grazoprevir potassiuM salt;2)-ether potassium salt (1:1);Grazoprevir (MK-5172) potassium salt;GRAZOPREVIR POTASSIUM SALT;MK5172 POTASSIUM SALT;MK 5172 POTASSIUM SALT;(1R,2S)-N-[[[(1R,2R)-2-[5-(3-Hydroxy-6-methoxy-2-quinoxalinyl)pentyl]cyclopropyl]oxy]carbonyl]-3-methyl-L-valyl-(4R)-4-hydroxy-L-prolyl-1-amino-N-(cyclopropylsulfonyl)-2-ethenylcCyclopropanecarboxamide cyclic (1-2)-ether potassium salt (1:1)
- CBNumber
- CB02666660
- Molecular Formula
- C38H49N6O9S.K
- Formula Weight
- 807.02
- MOL File
- 1206524-86-8.mol
MK 5172 potassiuM salt Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:100.0(Max Conc. mg/mL);124.22(Max Conc. mM)
- form
- Powder
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-1375
- Product name
- Grazoprevirpotassiumsalt
- Purity
- 99.40%
- Packaging
- 5mg
- Price
- $108
- Updated
- 2021/12/16
- Product number
- A3620
- Product name
- MK-5172potassiumsalt
- Packaging
- 1mg
- Price
- $126
- Updated
- 2021/12/16
- Product number
- CS-1375
- Product name
- Grazoprevirpotassiumsalt
- Purity
- 99.40%
- Packaging
- 10mg
- Price
- $168
- Updated
- 2021/12/16
- Product number
- CS-1375
- Product name
- Grazoprevirpotassiumsalt
- Purity
- 99.40%
- Packaging
- 50mg
- Price
- $540
- Updated
- 2021/12/16
- Product number
- CS-1375
- Product name
- Grazoprevirpotassiumsalt
- Purity
- 99.40%
- Packaging
- 100mg
- Price
- $780
- Updated
- 2021/12/16
MK 5172 potassiuM salt Chemical Properties,Usage,Production
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 potassiuM salt Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from MK 5172 potassiuM salt manufacturers
- Product
- MK 5172 potassiuM salt 1206524-86-8
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- ask
- Release date
- 2018-12-23