L-692,429 , CID121879

L-692,429 , CID121879

中文名称L-692,429 , CID121879
中文同义词化合物 T11798;化合物 L-692429
英文名称L 692429
英文同义词L 692429;MK 0751;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;L-692,429 , CID121879;L692429,L 692429;Butanamide, 3-amino-3-methyl-N-[(3R)-2,3,4,5-tetrahydro-2-oxo-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-1-benzazepin-3-yl]-;L-692429 free base
CAS号145455-23-8
分子式C29H31N7O2
分子量509.611
EINECS号
相关类别
Mol文件145455-23-8.mol
结构式L-692,429 , CID121879 结构式

L-692,429 , CID121879 性质

密度1.33±0.1 g/cm3(Predicted)
储存条件Store at -20°C
溶解度二甲基亚砜:50 mg/ml(98.12 mM)
酸度系数(pKa)4.14±0.10(Predicted)
形态固体
颜色白色至米白色

L-692,429 , CID121879 用途与合成方法

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)。

Growth hormone secretagogue (GHS)

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.

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/08/19HY-10957L-6924291 mg2181元
2024/08/19HY-10957L-692,429 , CID121879
L-692429
145455-23-85mg4800元

L-692,429 , CID121879 上下游产品信息

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