SR146131

Research use only, not for human use.

SR146131 (SR-146131) a small molecule positive allosteric modulator of the type 1 cholecystokinin receptor (CCK1R) with pEC50 of 10.34.

SR146131 (SR-146131) a small molecule positive allosteric modulator of the type 1 cholecystokinin receptor (CCK1R) with pEC50 of 10.34.

SR 146131 inhibits in the binding of [125I]-BH-CCK-8S to CCK1sites on 3T3-hCCK1 cell membranes with an IC50 value of 0.56 ± 0.10 nM. At much higher concentrations, SR 146131 also inhibits the binding of radiolabeled CCK to CCK2sites in CHO-hCCK2 membranes with an IC50 of 162 ± 27 nM. SR 146131 is a potent CCK1 agonist on several intracellular events linked to CCK1 receptor activation in various cell types: on [Ca2+]i release and IP1 formation, SR 146131 appears as a full CCK1 receptor agonist in the 3T3-hCCK1 cells, but a partial CCK1receptor agonist on MAPK activation and early gene expression in this cell line. SR 146131 also acts as a partial agonist in the two neuroblastoma cell lines.

SR 146131 completely inhibits gastric and gallbladder emptying in mice (ED50 of 66 and 2.7 μg/kg p.o., respectively). SR 146131 dose dependently reduces food intake in fasted rats (from 0.1 mg/kg p.o.), in nonfasted rats in which food intake has been highly stimulated by the administration of neuropeptide Y (1–36) (from 0.3 mg/kg p.o.), in fasted gerbils (from 0.1 mg/kg p.o.), and in marmosets maintained on a restricted diet (from 3 mg/kg p.o.). SR 146131 (10 mg/kg p.o.) also increases the number of Fos-positive cells in the hypothalamic paraventricular nucleus of rats. Locomotor activity of mice is reduced by orally administered SR 146131 (from 0.3 mg/kg p.o.).

SR-146131 | SR 146131

GPCR/G Protein

Cholecystokinin Receptor

Cholecystokinin Receptor

Metabolic Disease

——

221671-61-0

610.166

C32H36ClN3O5S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (409.73 mM)

O=C(O)CN1C(C(NC2=NC(C3=CC(OC)=C(Cl)C=C3OC)=C(CCC4CCCCC4)S2)=O)=CC5=C1C(C)=CC(C)=C5

2-(2-((4-(4-chloro-2,5-dimethoxyphenyl)-5-(2-cyclohexylethyl)thiazol-2-yl)carbamoyl)-5,7-dimethyl-1H-indol-1-yl)acetic acid

(-20℃)

With Ice Pack

≥ 2 years