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L-692429

CAS No. : 145455-23-8

MCE 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 K_i 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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