13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
聯(lián)系人:高小姐
電話:021-59541103 021-60443211
手機(jī):13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細(xì)地址：上海嘉定區(qū)嘉羅公路1661
化學(xué)性質(zhì)：
| 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 |
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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開 戶 行：中國銀行山東省分行營業(yè)部
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