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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Rev-ErbA-SR12418
SR12418

Chemical Structure : SR12418

CAS No.: 1801185-08-9

SR12418 (SR-12418)

货号: PC-22073Not For Human Use, Lab Use Only.

SR12418 (SR-12418) is a potent, selective REV-ERB ligand/agonist with IC50 of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively, in TR-FRET biochemical assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SR12418 (SR-12418) is a potent, selective REV-ERB ligand/agonist with IC50 of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively, in TR-FRET biochemical assay.
SR12418 is more potent than SR9009.
SR12418 also shows minimal off-target activity in a CEREP (Eurofins Scientific) panel screen of 84 G-protein coupled receptors, ion channels, and transporters.
SR12418 dose-dependently inhibits Il17a lucif-erase activity at REV-ERBα and REV-ERBβ and inhibitsTH17 cell differentiation without affecting viability or other T helper populations.
SR12418 potently represses TH17-mediated gene expression and Nfil3, which is consistent with REV-ERBα acting as a repressor at RORE and/or RevRE sites.
SR12418 (i.p., 50mg/kg, b.i.d.) potently suppresses the development and severity of MOG-induced EAE model, inhibits TH17-mediated autoimmunity.

物理化学性质&存储条件

分子量 483.58
分子式 C31H30FNO3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

[(3S)-3-[[4-(1,1-Dimethylethoxy)phenoxy]methyl]-6-fluoro-3,4-dihydro-2(1H)-isoquinolinyl]-1-naphthalenylmethanone

参考文献

1. Amir M, et al. Cell Rep. 2018 Dec 26;25(13):3733-3749.e8.

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