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標(biāo)簽:SR 1555 (hydrochloride)
聯(lián)系人:高小姐
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化學(xué)性質(zhì):
規(guī)格 | 1mg 5mg 10mg 25mg |
CAS |
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別名 |
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化學(xué)名 | 1-(4-((4'-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-[1,1'-biphenyl]-4-yl)methyl)piperazin-1-yl)ethanone, monohydrochloride |
分子式 | C22H22F6N2O2 HCl |
分子量 | 496.9 |
溶解度 | ≤1.6mg/ml in ethanol;3mg/ml in DMSO;5mg/ml in dimethyl formamide |
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:
SR 1555 is a novel RORγ-specific synthetic ligand [1].
Retinoic acid receptor-related nuclear receptor (ROR) belongs to the nuclear receptor superfamily, a group of structurally related, ligand-dependent transcription factors. RORs function as key regulators of many physiological processes that occur during embryonic development and in the adult [2]. RORγ plays a dominant role in T cell differentiation, particularly in the development of TH17 cells, which are implicated in autoimmune diseases such as multiple sclerosis and rheumatoid arthritis [3].
In vitro: In a GAL4-NR chimeric co-transfection assay, SR1555 was devoid of LXR, FXR, and RORα activity, but it dose-dependently repressed the activity at RORγ with an IC50 of ≈ 1.5 μM. In competitive radioligand binding assays, SR1555 bound to RORγ with an IC50 of 1 μM. SR1555 specifically targeted RORγ and inhibited its transcriptional activity leading to suppression of IL-17 gene expression. EL4 cells treated SR1555 (10 μM) for 24 h inhibited Il17a gene expression by greater than 70%, demonstrating that SR1555 could inhibit the expression of this TH17 mediated cytokine [1]. SR1555 not only inhibited TH17 cell development and function but also increased the frequency of T regulatory cells [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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