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SR3335
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产品介绍
产品介绍
产品信息
抗原名称
ROR
商品描述
SR3335 is a selective ROR?? synthetic ligand, directly binds to ROR??, but not other RORs, and functions as a selective partial inverse agonist of ROR?? in cell-based assays.
分子量
405.34
纯度
>98%
可溶性
10 mM in DMSO
In vitro(体外研究)
SR3335 is a selective RORα partial inverse agonist. In a biochemical radioligand binding assay using 25-hydroxycholesterol as a label it is clear that unlabeled SR3335 dose-dependently competes for binding to the RORα LBD. The Ki is calculated as 220 nM using the Cheng-Prusoff equation. In a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand binding domain cotransfection assay, SR3335 significantly inhibits the constitutive transactivation activity of RORα (IC50=480 nM)(partial inverse agonist activity), but has no effect on the activity of LXRα and RORγ.
In vivo(体内研究)
Pharmacokinetic studies indicate that SR3335 displays reasonable exposure following an i.p. injection into mice. The ability of SR3335 is assessed to suppress gluconeogenesis using a diet induced obesity (DIO) mouse model where the mice where treated with 15 mg/kg b.i.d., i.p. for 6-days followed by a pyruvate tolerance test. SR3335 treated mice displays lower plasma glucose levels following the pyruvate challenge consistent with suppression of gluconeogenesis. Importantly, mice treated with SR3335 displayed no difference in body weight or food intake after 7-days of treatment with SR3335.
背景
别名
ML-176, SR 3335, SR-3335, ML176, ML 176
分子式
C13H9F6NO3S2
CAS号
293753-05-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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