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Grazoprevir is a hepatitis C virus protease inhibitor developed for the treatment of hepatitis C. It suppresses NS3 and NS4A, which play a role in the virus splitting its polyprotein into the functional virus proteins. Grazoprevir is often used in combination with elbasvir or ribavirin. Uses: Antiviral agents. Synonyms: Cyclopropanecarboxamide, 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-ethenyl-, cyclic (1?2)-ether, (1R,2S)-; Grazoprevir; (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-ethenylcyclopropanecarboxamide Cyclic (1?2)-Ether. Grades: >98%. CAS No. 1350514-68-9. Molecular formula: C38H50N6O9S. Mole weight: 766.91.
MK-5172 hydrate
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 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. Uses: Antiviral agents. Synonyms: (33R,35S,91R,92R,5S)-5-(tert-butyl)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxamide hydrate; MK-5172; MK 5172; MK5172; Grazoprevir; Grazoprevir hydrate; trade name: Zepatier?. Grades: >98%. CAS No. 1350462-55-3. Molecular formula: C38H52N6O10S. Mole weight: 784.92.
MK-5172 intermediate
Cas No. 1206524-85-7.
MK-5172 potassium salt
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 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. Synonyms: Grazoprevir potassium salt; MK5172 potassium salt; MK 5172 potassium salt. Grades: >98%. CAS No. 1206524-86-8. Molecular formula: C38H49KN6O9S. Mole weight: 804.99.
MK-5172 sodium salt
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 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. Synonyms: Grazoprevir sodium salt; MK5172 sodium salt; MK 5172 sodium salt. Grades: >98%. CAS No. 1425038-27-2. Molecular formula: C38H49N6NaO9S. Mole weight: 788.89.
Grazoprevir
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K i s of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively [1] [2]. Grazoprevir inhibits SARS-CoV-2 3CL pro activity [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MK-5172. CAS No. 1350514-68-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15298.
Grazoprevir hydrate
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K i s of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively [1] [2]. Grazoprevir hydrate inhibits SARS-CoV-2 3CL pro activity [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MK-5172 hydrate. CAS No. 1350462-55-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15298B.
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