L-692429

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

L-692429 (MK-0751) 是一种苯并内酰胺的衍生物，也是一种非肽基生长激素促分泌素 (GHS) 激动剂。L-692429 以 Ki 值为 63 nM 来结合 G 蛋白偶联受体 (G protein-coupled receptor)。

L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM.

L-692429 stimulates intracellular calcium release, inositol phosphate (IP) turnover, cAMP-responsive element binding protein (CREB) activity, serum-responsive element activity and bioluminescence resonance energy transfer (BRET) activity with EC50 values of 26 nM, 47 nM, 60 nM, 63 nM and 58 nM, respectively.HeLa-T4 cells transiently expressing the flag epitope-tagged growth hormone secretagogue (GHS) receptor are treated with L-692429. The release of intracellular calcium is measured using fluorometry with the calcium indicator dye fluo-3/AM. Untransfected HeLa-T4 cells are unresponsive to L-692429 treatment, whereas HeLa-T4 cells transiently expressing GHS receptors demonstrate an increase in fluorescent emission after L-692429 treatment. A significant increase in luciferase activity after L-692429 treatment is seen, suggesting that activation of the GHS receptor stimulates the MAPK pathway.

When tested in anesthetized rats (Wistar rats), L-756867 inhibits L-692429 (100 μg/kg)-stimulated GH secretion in a dose-dependent manner. Complete inhibition is observed at an i.v. dose of 100 μg/kg of L-756867.

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GPCR/G Protein

GPCR19

GPCR19 | GHSR

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145455-23-8

509.614

C29H31N7O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (98.12 mM; 超声助溶 )

CC(C)(N)CC(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(cc2)-c2ccccc2-c2nn[nH]n2)C1=O

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(-20℃)

With Ice Pack

≥ 2 years