SR27897

生物活性靶点体外研究体内研究 SR27897 试剂级价格

SR27897

CAS号:136381-85-6
英文名:SR27897
中文名:SR27897
CBNumber:CB11074591
分子式:C20H14ClN3O3S
分子量:411.86
MOL File:136381-85-6.mol

SR27897化学性质

密度 :1.49±0.1 g/cm3(Predicted)
储存条件 :Desiccate at +4°C
溶解度 :DMSO: ≥10mg/mL at warmed to 60°C
酸度系数(pKa) :4.00±0.10(Predicted)
形态 :powder
颜色 :white to tan

安全信息

危险品标志 :T
危险类别码 :25-41
安全说明 :26-45
危险品运输编号 :UN 2811 6.1 / PGIII
WGK Germany :3

SR27897性质、用途与生产工艺

生物活性 Lintitript (SR 27897) 是一种高效，选择性，口服活性，竞争性和非肽类 CCK1 受体拮抗剂，EC50 为 6 nM，Ki 为 0.2 nM。Lintitript 对 CCK1 的选择性比对 CCK2 受体的选择性高 33 倍以上 (EC50值为 200 nM)。Lintitript 增加瘦素的血浆浓度和食物摄入以及胰岛素的血浆浓度。
靶点

EC50: 6 nM (cholecystokinin (CCK1) receptor); Ki: 0.2 nM (cholecystokinin (CCK1) receptor)
体外研究

In vitro, Lintitript (SR 27897) is a competitive antagonist of cholecystokinin (CCK)-stimulated amylase release in isolated rat pancreatic acini (pA ₂ = 7.50) and of CCK-induced guinea pig gall bladder contractions (pA ₂ = 9.57).
Lintitript produces concentration dependent inhibition of [ ¹²⁵ I]CCK binding to CCK1 receptor sites in the rat pancreas (IC ₅₀ value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC ₂ value of 479 nM). Lintitript inhibits [ ¹²⁵ I]gastrin binding to gastrin receptors. Lintitript (0.5 nM) increases the dissociation constant of CCK for the CCK A receptor (K _d = 1.8 to 7.2 nM) without modifying the maximum number of receptors (B _max = 1800 to 1770 fmol/mg).
体内研究

Lintitript (SR 27897; 1 mg/kg, i.v.) completely reverses the CCK-induced amylase secretion. Lintitript also inhibits CCK-induced gastric and gallbladder emptying in mice (ED ₅₀ s = 3 and 72 μg/kg, respectively). Lintitript is also very active (ED ₅₀ = 27 μg/kg p.o.) in the gall bladder emptying protocol with egg yolk as an inducer of endogenous CCK release.