(αR,8aS)-GSK1614343,1092476-84

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

(αR,8aS)-GSK1614343

CAS No. : 1092476-84-0

MCE 国际站：(αR,8aS)-GSK1614343

产品活性：(αR,8aS)-GSK1614343 (compound 18a, d2) 是环化胃促生长素拮抗剂，pIC₅₀ 值为 8.4. (αR,8aS)-GSK1614343 对 hGHSR1a 具有竞争性拮抗作用，平均 pK_b 值为 8.06。

研究领域：GPCR/G Protein

作用靶点：GHSR

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.

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 IC50 value of ≥10 μM.}

相关产品：Anamorelin  |  TC-G-1008  |  Ibutamoren Mesylate  |  PF-5190457  |  JMV 2959  |  TM-N1324  |  Capromorelin Tartrate  |  YIL781 hydrochloride  |  Relamorelin TFA  |  AZP-531  |  des-​Gln14-​Ghrelin  |  Human growth hormone-releasing factor TFA  |  L-692429  |  L-692585  |  AZ-GHS-22  |  BMS-604992  |  des-​Gln14-​Ghrelin TFA  |  Emoghrelin  |  Ghrelin receptor full agonist-2  |  GHRF, bovine  |  GHRF, porcine  |  GSK1614343  |  GSK894281  |  GSK894490A

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds