產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg 200mg
CAS	1246525-60-9
別名	SR 1078;SR-1078
化學(xué)名	N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-4-(trifluoromethyl)benzamide
分子式	C17H10F9NO2
分子量	431.25
溶解度	≥ 43.2 mg/mL in DMSO, ≥ 43.4 mg/mL in EtOH
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：

SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR) RORα and RORγ with IC50 values of both 1-3 μM [1].

RORα and RORγ are two members of nuclear receptor superfamily, which possesses a highly conserved DNA-binding and a ligand-binding domain. These two receptors are considered to play important roles in the regulation of metabolism and the function of immune system [1].

SR1078 is a selective RORα and RORγ agonist, which activate RORα and RORγ directed transcription via inducing conformational changes [1].

SR1078 selectively targets on RORα and RORγ as an agonist but not on LXR and FXR [1]. It was shown that SR1078 was able to stimulate ROR activity and subsequent ROR-directed mRNA expression. When HepG2 cells were treated with SR1078 for 24h, the ROR directed reporter gene FG21 mRNA level was increased by 3-fold, while another reporter gene G6Pase was increased by 2-fold [1].

In mouse model, i.p. injection of 10 mg/kg SR1078 for 1 hr resulted in 3.6 μM plasma concentration., and after 8 hr the concentration still sustained at 800 nM. i.p. injection of 10 mg/kg SR1078 for 2 hr resulted in significantly increased level of mRNA of reporter gene G6Pase and FG21 [1].

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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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