SR-31747 free base 是一种具有免疫抑制和抗炎特性的 sigma 配体。SR-31747 free base 通过抑制固醇异构酶来阻止细胞增殖。
生物活性
SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase.
性状
Liquid
IC50 & Target[1][2]
Sigma ligand
体外研究(In Vitro)
SR-31747 blocks the proliferation of lymphocytes at a concentration of 10 nM. SR-31747 is capable of inhibiting T-cell proliferation when added as late as 24 h after activation. SR-31747 arrests proliferation in yeast cells in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
In vivo, SR-31747 dramatically blocks lipopolysaccharide-induced production of IL-1, IL-6 and TNF-α in a dose-dependent manner (ED 50 , 2 mg/kg). SR-31747 probably abrogated monokine production through an indirect mechanism that involves endogenous corticosteroids. This conclusion was supported by in vivo experiments that shows that: 1) ablation of corticosteroids by use of Mifepristone or adrenalectomy suppress the effect of SR-31747; 2) administration of SR-31747 induces an enhancement of the corticosterone level. SR-31747 improves the survival of animals with endotoxinic shock as a result of monokine inhibition. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Derocq JM, et al. In vivo inhibition of endotoxin-induced pro-inflammatory cytokines production by the sigma ligand SR 31747. J Pharmacol Exp Ther. 1995 Jan;272(1):224-30.[2]. Silve S, et al. The immunosuppressant SR 31747 blocks cell proliferation by inhibiting a steroid isomerase in Saccharomyces cerevisiae. Mol Cell Biol. 1996 Jun;16(6):2719-27.
溶解度数据
In Vitro: DMSO : 5 mg/mL (13.89 mM; Need ultrasonic)配制储备液