產(chǎn)品目錄

規(guī)格	250mg 500mg
CAS	221671-61-0
別名	N/A
化學(xué)名	N/A
分子式	C32H36ClN3O5S
分子量	610.16
溶解度	Soluble in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.

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[1].

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.)[1].

[1]. Bignon E, et al. SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther. 1999 May;289(2):742-51. [2]. Bignon E, et al. SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. II. In vivo pharmacological characterization. J Pharmacol Exp Ther. 1999 May;289(2):752-61.

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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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