Product Name :
Lintitript
Description:
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.
CAS:
136381-85-6
Molecular Weight:
411.86
Formula:
C20H14ClN3O3S
Chemical Name:
2-(2-[4-(2-chlorophenyl)-1,3-thiazol-2-yl]carbamoyl-1H-indol-1-yl)acetic acid
Smiles :
OC(=O)CN1C(=CC2=CC=CC=C12)C(=O)NC1=NC(=CS1)C1=CC=CC=C1Cl
InChiKey:
ILNRQFBVVQUOLP-UHFFFAOYSA-N
InChi :
InChI=1S/C20H14ClN3O3S/c21-14-7-3-2-6-13(14)15-11-28-20(22-15)23-19(27)17-9-12-5-1-4-8-16(12)24(17)10-18(25)26/h1-9,11H,10H2,(H,25,26)(H,22,23,27)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Denosumab custom synthesis
Shelf Life:
≥12 months if stored properly.Lumateperone site
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:33155853
Additional information:
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.|Product information|CAS Number: 136381-85-6|Molecular Weight: 411.86|Formula: C20H14ClN3O3S|Chemical Name: 2-(2-[4-(2-chlorophenyl)-1,3-thiazol-2-yl]carbamoyl-1H-indol-1-yl)acetic acid|Smiles: OC(=O)CN1C(=CC2=CC=CC=C12)C(=O)NC1=NC(=CS1)C1=CC=CC=C1Cl|InChiKey: ILNRQFBVVQUOLP-UHFFFAOYSA-N|InChi: InChI=1S/C20H14ClN3O3S/c21-14-7-3-2-6-13(14)15-11-28-20(22-15)23-19(27)17-9-12-5-1-4-8-16(12)24(17)10-18(25)26/h1-9,11H,10H2,(H,25,26)(H,22,23,27)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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). Lintitript produces concentration dependent inhibition of [125I]CCK binding to CCK1 receptor sites in the rat pancreas (IC50 value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC2 value 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).|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.|Products are for research use only. Not for human use.|