136381-85-6
Chemical Structure
Lintitript
Synonym(s): SR 27897
- CAS No.: 136381-85-6
- Formula:C20H14ClN3O3S
- Molecular Weight:411.86
IUPAC Name: 2-(2-((4-(2-chlorophenyl)thiazol-2-yl)carbamoyl)-1H-indol-1-yl)acetic acid
InChIKey: ILNRQFBVVQUOLP-UHFFFAOYSA-N
SMILES: O=C(O)CN1C(C(NC2=NC(C3=CC=CC=C3Cl)=CS2)=O)=CC4=C1C=CC=C4
Biological Activity: Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin[1][2][3].
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Lintitript | 99.0% | Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin. | ||||||||||||||||||||
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Lintitript (Standard) | ≥98% | Lintitript (Standard) (SR 27897 (Standard)) is the analytical standard of Lintitript (HY-101764). This product is intended for research and analytical applications. Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords