| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Lintitript 是 CCK1的选择性拮抗剂,对 CCK1和 CCK2的 EC50s 为6 nM 和200 nM。对 CCK1的 Ki 值为0.2 nM。
产品描述 | Lintitript is a selective antagonist of CCK1 with EC50s of 6 nM and 200 nM for CCK1 and CCK2. The Ki value is 0.2 nM for CCK1. |
靶点活性 | CCK1:(EC50)6 nM, cholecystokinin CCK1 receptor:(ki)0.2 nM |
体外活性 | Lintitript inhibited the CCK 2 site in guinea pig cortex with an IC2 of 479 nM. lintitript (0.5 nM) increased the dissociation constant of CCK on CCKA receptors with Kds between 1.8 and 7.2 nM without altering the maximum number of receptors. lintitript antagonized CCK-stimulated isolated rat pancreatic follicles in (amylase release and CCK-induced gallbladder contraction in guinea pigs with pA2s of 7.50 and 9.57). lintitript inhibited the binding of [125I]CCK to the rat pancreatic CCK1 receptor site with IC50 of 0.58 nM in a concentration-dependent manner[1]. |
体内活性 | Lintitript (1 mg/kg, i.v.) completely reversed CCK-induced amylase secretion. lintitript inhibited CCK-induced gastric and gallbladder emptying in mice with ED50s of 3 μg/kg and 72 μg/kg. lintitript (p.o.) was active in the gallbladder emptying protocol of egg yolk-induced endogenous CCK release, with an ED50 of 27 μg/kg [1]. |
别名 | SR 27897, 林替曲特 |
分子量 | 411.86 |
分子式 | C20H14ClN3O3S |
CAS No. | 136381-85-6 |
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 90 mg/mL (218.5 mM), Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Lintitript 136381-85-6 GPCR/G Protein cholecystokinin SR 27897 林替曲特 Inhibitor inhibitor inhibit