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编 号:F756392
分子式:C29H33ClN6O2S
分子量:565.13
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生物活性:
PF-6870961 hydrochloride is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 hydrochloride inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 hydrochloride also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM.

体内研究:
PF-6870961 hydrochloride (40 mg/kg;腹腔注射) 抑制饱食和禁食大鼠的食物摄入。Animal Model:Satiated and fasted rats model
Dosage:2.5 mg/kg, 10 mg/kg, and 40 mg/kg
Administration:Intraperitoneal injection
Result:Significantly reduced food intake at 40 mg/kg.
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