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Lintitript
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lintitript图片
CAS NO:136381-85-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
SR 27897
产品介绍
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。
生物活性

Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptidecholecystokinin (CCK1) receptorantagonist with anEC50of 6 nM and aKiof 0.2 nM. Lintitript displays >33-fold selectivity more selective forCCK1than CCK2 receptors (EC50value of 200 nM). Lintitript increases plasma concentration ofleptinand food intake as well as plasma concentration ofinsulin[1][2][3].

IC50& Target

EC50: 6 nM (cholecystokinin (CCK1) receptor)[2]; Ki: 0.2 nM (cholecystokinin (CCK1) receptor)[1]

体外研究
(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)[1].
Lintitript produces concentration dependent inhibition of [125I]CCK binding to CCK1 receptor sites in the rat pancreas (IC50value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC2value 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)[1].

体内研究
(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[1].

分子量

411.86

性状

Solid

Formula

C20H14ClN3O3S

CAS 号

136381-85-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(242.80 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4280 mL12.1400 mL24.2801 mL
5 mM0.4856 mL2.4280 mL4.8560 mL
10 mM0.2428 mL1.2140 mL2.4280 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。