Bioactivity | SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase[1][2]. | |||||||||
Target | Sigma ligand | |||||||||
Invitro | 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[2]. | |||||||||
In Vivo | In vivo, SR-31747 dramatically blocks lipopolysaccharide-induced production of IL-1, IL-6 and TNF-α in a dose-dependent manner (ED50, 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[1]. | |||||||||
Name | SR-31747 free base | |||||||||
CAS | 132173-06-9 | |||||||||
Formula | C23H34ClN | |||||||||
Molar Mass | 359.98 | |||||||||
Appearance | Liquid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [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. |