Devazepide|103420-77-5|(地伐西匹; L-364,718; MK-329)-陌孚医药/Medlife

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Devazepide (Synonyms: 地伐西匹; L-364,718; MK-329)

目录号: PL01559 纯度: ≥98%

CAS No. :103420-77-5

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中文名称	Devazepide
中文别名	地伐西匹
英文名称	Devazepide
英文别名	1H-Indole-2-carboxamide,N-[(3S)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-;Devazepide;N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamide;Devazepida;Devazepidum;MK-329;(S)-N-(2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)indole-2-carboxamide;MK 329;L-364718;EVAZEPIDE, PANOS;(3S)-1-Methyl-3-[(1H-indol-2-yl)carbonylamino]-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one;N-[(3S)-2,3-DIHYDRO-1-METHYL-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-1H-INDOLE-2-CARBOXAMIDE;L-364,718;DEVAZEPIDE
Cas No.	103420-77-5
分子式	C₂₅H₂₀N₄O₂
分子量	408.45
包装储存	-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情	Devazepide (L-364,718) 是一种有效、竞争性、选择性、可口服的非肽类胆囊收缩素受体 (cholecystokinin (CCK) receptor) 拮抗剂，对大鼠胰腺、牛胆囊和豚鼠大脑 CCK 受体的 IC₅₀ 值分别为 81 pM，45 pM 和 245 nM。Devazepide (L-364,718) 对肠胃疾病有效。
生物活性	Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC 50 s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders.
性状	Solid
IC50 & Target[1][2]	IC50: 45 pM (Rat pancreatic CCK receptor), 81 pM (Bovine gallbladder CCK receptor), 245 nM (Guinea pig brain CCK receptor)
体内研究(In Vivo)	Devazepide (oral gavage; 4 mg/kg; twice per day) significantly accelerates cholesterol crystallization and crystal growth to microlithiasis, and the formation of gallstones in mice. Devazepide (intraperitoneal injection; 0.1-1 mg/kg) has opposite effects on spontaneous locomotor activity, and on caerulein- and apomorphine-induced hypomotility in the mouse. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献	[1]. Chang RS, et al. Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist. Proc Natl Acad Sci U S A. 1986 Jul;83(13):4923-6. [2]. Helen H Wang, et al. The cholecystokinin-1 receptor antagonist devazepide increases cholesterol cholelithogenesis in mice. Eur J Clin Invest

溶解度数据	In Vitro: DMSO : 200 mg/mL (489.66 mM; Need ultrasonic)配制储备液

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