| 名称 | L-692429 |
| 描述 | L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist and benzolactam derivative, known for reversing glucocorticoid-induced inhibition of GH secretion. L-692429 exhibits high affinity for the G protein-coupled receptor and is useful in studying acromegaly and obesity. |
| 体外活性 | L-692429, a chemical compound, activates various cellular mechanisms, including 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[2]. In experiments involving HeLa-T4 cells, those transiently expressing flag epitope-tagged growth hormone secretagogue (GHS) receptor and treated with L-692429 show a measurable increase in intracellular calcium, as detected by fluorometry using fluo-3/AM calcium indicator dye. This response is absent in untransfected HeLa-T4 cells, indicating the specificity of L-692429 for GHS receptor-expressing cells. Moreover, L-692429 treatment significantly enhances luciferase activity in these cells, suggesting that GHS receptor activation triggers the MAPK pathway[1]. |
| 体内活性 | In anesthetized Wistar rats, L-756867 dose-dependently suppresses GH secretion stimulated by L-692429 (100 μg/kg), with complete inhibition achieved at an intravenous dose of 100 μg/kg of L-756867[3]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 40 mg/mL (78.49 mM), Sonication is recommended.
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| 关键字 | MK 0751 | L692429 | MK0751 | L 692429 | L-692429 |
| 相关产品 | Ibutamoren Mesylate | Anamorelin | Ursodeoxycholic acid sodium | TC-G 1005 | Deoxycholic acid | Triamterene | Deoxycholic acid sodium salt | NF-56-EJ40 hydrochloride | Hyodeoxycholic acid | PEN (human) aceate | SB756050 | Cortistatin-8 acetate |
| 相关库 | 经典已知活性库 | 已知活性化合物库 | GPCR靶点分子库 |
United States
