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145455-23-8

中文名称 L-692,429 , CID121879
英文名称 L 692429
CAS 145455-23-8
分子式 C29H31N7O2
分子量 509.6
MOL 文件 145455-23-8.mol
145455-23-8 结构式 145455-23-8 结构式

基本信息

中文别名
化合物 T11798
英文别名
MK 0751
L 692429
L-692,429 , CID121879
3-amino-3-methyl-N-[(3R)-2-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-4,5-dihydro-3H-1-benzazepin-3-yl]butanamide

物理化学性质

密度1.33±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 50 mg/mL (98.12 mM)
酸度系数(pKa)4.14±0.10(Predicted)
形态Solid
颜色White to off-white
L-692,429 , CID121879价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-10957L-692429145455-23-81 mg2181元
2025/05/22HY-10957L-692,429 , CID121879
L-692429
145455-23-85mg4800元
2025/05/22HY-10957L-692,429 , CID121879
L-692429
145455-23-810mM * 1mLin DMSO5381元

常见问题列表

生物活性
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)。
靶点

Growth hormone secretagogue (GHS)

体外研究

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 EC 50 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.

体内研究

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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