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Lintitript

Catalog No. T15759   CAS 136381-85-6
Synonyms: SR 27897

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.

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Lintitript, CAS 136381-85-6
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 cholecystokinin CCK1 receptor:(ki)0.2 nM, CCK1:(EC50)6 nM
In vitro 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].
In vivo 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].
Synonyms SR 27897
Molecular Weight 411.86
Formula C20H14ClN3O3S
CAS No. 136381-85-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 90 mg/mL (218.5 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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.

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