(αR,8aS)-GSK1614343 (C007B-357700)

(αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC 50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pK b value of 8.06.In Vitro(αR,8aS)-GSK1614343 (0.1-1μM) demonstrats a surmountable and competitive antagonism of hGHSR1a with a mean p K B value of 8.06. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In Vivo(αR,8aS)-GSK1614343 (10 mg/kg; i.v. once) inhibits GH release induced by exogenous ghrelin administration . (αR,8aS)-GSK1614343 (i.v. and p.o.) exhibits good oral bioavailability (F=46%), a limited clearance in blood (Cl b =28 mL/min/kg) and a suitable half-life (5.0 h). In terms of rat brain penetration, a brain to blood AUC ratio of 2.2 is observed after p.o. administration of the compound at a dose of 3 mg/kg . (αR,8aS)-GSK1614343 exhibits a clean profile in terms of inhibition potential for the major human CYP450 isoforms with IC 50 value of ≥10 μM . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:Solid. Specification: 0.99 Molecular Formula: C22H23F6N5O Molecular Weight: 487.44

UPC:

41116010

Condition:

New

Weight:

1.06 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

G649664-10mg

CAS:

1092476-84-0

Product Size:

10mg