产品
编 号:F167945
分子式:C32H37N7O3
分子量:567.68
产品类型
结构图
CAS No: 145455-35-2
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产品详情
生物活性:
L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.
体内研究:
L-692585 (0.01-0.1 mg/kg; i.v. once daily for 2 weeks) increases peak plasma GH levels and total GH release.L-692585 (0.005-0.1 mg/kg; a single i.v.) significantly increases peak GH concentrations 4.3-fold at a dose of 0.005 mg/kg, 7-fold at a dose of 0.02 mg/kg, and 21-fold at a dose of 0.10 mg/kg in vivo.Animal Model:Beagles (1-1.5 years old ; weighting 8.5-16.0 kg)
Dosage:0.01, 0.1 mg/kg
Administration:I.v. once daily for 2 weeks
Result:Increased the peak plasma GH levels and total GH release on days 1, 8 and 15 in a dose-dependent manner, and no desensitization was evident.
体外研究:
L-692585 (10 μM; 2 min) produces a prompt transient increase in [Ca2+]i, following by the sustained decline to a plateau above the basal level in GH cells.L-692585 (0.01-10 μM; 2 min) induces release of growth hormone (GH) in a dose-dependent manner from isolated porcine somatotropes.L-692585 (100 nM) signi?cantly increases the number and size of plaques, and it also causes a signi?cant increase in total secretion index (TSI) .