Structure
Lintitript, Inhibitor
Lintitript
Purity
98.00%
Synonyms
Lintitript; SR 27897; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
Formula
C20H14ClN3O3S
SMILES
O=C(O)CN1C(C(NC2=NC(C3=CC=CC=C3Cl)=CS2)=O)=CC4=C1C=CC=C4
CAS Number
136381-85-6
Target & IC50
CCK1: ic50 6nM (EC50)
cholecystokinin CCK1 receptor: ic50 0.2nM (ki)
cholecystokinin CCK1 receptor: ic50 0.2nM (ki)
In Vitro
Lintitript inhibits [125I]gastrin binding to gastrin receptors. Lintitript 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). Lintitript (0.5nM) increases the dissociation constant of CCK for the CCK A receptor (Kd = 1.8 to 7.2nM) without modifying the maximum number of receptors (Bmax = 1800 to 1770 fmol/mg). Lintitript produces concentration-dependent inhibition of [125I]CCK binding to CCK1 receptor sites in the rat pancreas (IC50: 0.58nM) and also to CCK 2 sites in the guinea pig cortex (IC2: 479nM) [1].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for Lintitript, inhibitor
Lintitript is an orally active, competitive, and non-peptide cholecystokinin (CCK1) receptor antagonist (EC50: 6nM; Ki: 0.2nM). Lintitript shows > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50: 200nM).
Product Categories/Family for Lintitript, inhibitor
References
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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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Product Notes
The Lintitript (Catalog #AAA5755105) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Lintitript, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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