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编 号:F757145
分子式:C29H19F9IN3O5
分子量:787.37
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生物活性:
RXFP2 agonist 2 is a selective,orally active and allosteric RXFP2 agonist with an EC50 value of 0.38 μM. RXFP2 agonist 2 induces osteoblast mineralization. RXFP2 agonist 2 increases bone formation in female mice. RXFP2 agonist 2 has the potential for the research of osteoporosis.

体内研究:
RXFP2 agonist 2 (10 mg/kg; p.o.; 每周 3 次,8 周) 促进雌性小鼠骨形成。Animal Model:8-week-old WT C57BL/6?J female mice
Dosage:3 mg/kg for i.v.; 10 mg/kg for p.o.
Administration:I.v. or p.o.
Result:Exhibited a half-life of between 4-6.5?h depending on the route of administration, with no accumulation at 10?mg/kg, and oral bioavailability around 25-31%.
Animal Model:8-week-old WT C57BL/6?J female mice
Dosage:10 mg/kg
Administration:P.o.; 3 times per week for 8 weeks
Result:Increased bone formation in mouse with significantly increased in Tb.N and Tb.Th, and increased BV/TV and decreased Tb.Sp.

体外研究:
RXFP2 agonist 2 (Compound 6641) (1, 3, 5 μM; 14 天) 在 3 和 5 μM 诱导成骨细胞矿化,对 HCO 细胞无细胞毒性。
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