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CAS No. : 145455-23-8
MCE 国际站:L-692429
产品活性: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)。
研究领域:GPCR/G Protein
作用靶点:GHSR
In Vitro: 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.
In Vivo: 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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