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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
SR 27897
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
136381-85-6
- 规格:
10 mM * 1 mL/5 mg/10 mg/25 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1491.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥1355.0 |
| 规格: | 10 mg | 产品价格: | ¥2165.0 |
| 规格: | 25 mg | 产品价格: | ¥4330.0 |
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Lintitript
CAS No. : 136381-85-6
MCE 国际站:Lintitript
产品活性: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。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Cholecystokinin Receptor
In Vitro: In vitro, Lintitript (SR 27897) is a competitive antagonist of cholecystokinin (CCK)-stimulated amylase release in isolated rat pancreatic acini (pA2 = 7.50) and of CCK-induced guinea pig gall bladder contractions (pA2 = 9.57).
Lintitript produces concentration dependent inhibition of [125I]CCK binding to CCK1 receptor sites in the rat pancreas (IC50 value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC2 value of 479 nM). Lintitript inhibits [125I]gastrin binding to gastrin receptors. Lintitript (0.5 nM) increases the dissociation constant of CCK for the CCK A receptor (Kd = 1.8 to 7.2 nM) without modifying the maximum number of receptors (Bmax = 1800 to 1770 fmol/mg).
In Vivo: 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 (ED50s = 3 and 72 μg/kg, respectively). Lintitript is also very active (ED50 = 27 μg/kg p.o.) in the gall bladder emptying protocol with egg yolk as an inducer of endogenous CCK release.
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