MK 5172 potassiuM salt Struktur

MK 5172 potassiuM salt

Bezeichnung:MK 5172 potassiuM salt

CAS-Nr1206524-86-8

Englisch Name:MK 5172 potassiuM salt

CBNumberCB02666660

SummenformelC38H49N6O9S.K

Molgewicht807.02

MOL-Datei1206524-86-8.mol

MK 5172 potassiuM salt physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	DMSO:100.0(Max Conc. mg/mL);124.22(Max Conc. mM)
Aggregatzustand	Powder
Farbe	White to off-white

MK 5172 potassiuM salt Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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