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Lintitript

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Chemical Structure| 136381-85-6 同义名 : SR 27897
CAS号 : 136381-85-6
货号 : A1209511
分子式 : C20H14ClN3O3S
纯度 : 99%+
分子量 : 411.861
MDL号 : MFCD00868618
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(254.94 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Lintitript, also known as SR 27897, is a potent, selective, orally active, competitive non-peptide antagonist of the CCK1 receptor, with an EC50 of 6 nM and a Ki of 0.2 nM. Its selectivity for the CCK1 receptor is 33 times greater than that for the CCK2 receptor (EC50 of 200 nM). Lintitript increases plasma concentrations of leptin and food intake as well as insulin[1][2][3]. Lintitript antagonizes CCK-stimulated amylase release in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced contractions in guinea pig gall bladder (pA2 = 9.57). It inhibits the binding of [125I]CCK to CCK1 receptor sites in rat pancreas (IC50 = 0.58 nM) and to CCK2 sites in guinea pig cortex (IC50 = 479 nM) in a concentration-dependent manner. Lintitript also inhibits the binding of [125I]gastrin to gastrin receptors. At 0.5 nM, Lintitript increases the dissociation constant (Kd) for CCK from the CCK A receptor (Kd = 1.8 to 7.2 nM) without altering the maximum number of receptors (Bmax = 1800 to 1770 fmol/mg)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.14mL

2.43mL

1.21mL

24.28mL

4.86mL

2.43mL
参考文献

[1]Gully D, et al. Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors. Eur J Pharmacol. 1993 Feb 23;232(1):13-9.

[2]Gouldson P, et al. Contrasting roles of leu(356) in the human CCK(1) receptor for antagonist SR 27897 and agonist SR 146131 binding. Eur J Pharmacol. 1999 Nov 3;383(3):339-46.

[3]Cano V, et al. Regulation of leptin distribution between plasma and cerebrospinal fluid by cholecystokinin receptors. Br J Pharmacol. 2003 Oct;140(4):647-52.