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编 号:F756391
分子式:C29H32N6O2S
分子量:528.67
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生物活性:
PF-6870961 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 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM.

体内研究:
PF-6870961 (40 mg/kg; i.p.) suppresses food intake in both satiated and fasted rats.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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