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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
(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