推荐产品
产品名称
REV-ERB激动剂 II,SR9009, The REV-ERB Agonist II, SR9009 controls the biological activity of REV-ERB. This small molecule/inhibitor is primarily used for Biochemicals applications.
质量水平
方案
≥96% (HPLC)
表单
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
dark brown
溶解性
DMSO: 50 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
ClC(C=C1)=CC=C1CN(CC2=CC=C(S2)[N+]([O-])=O)CC3CN(C(OCC)=O)CC3
InChI
1S/C20H24ClN3O4S/c1-2-28-20(25)23-10-9-16(13-23)12-22(11-15-3-5-17(21)6-4-15)14-18-7-8-19(29-18)24(26)27/h3-8,16H,2,9-14H2,1H3
InChI key
MMJJNHOIVCGAAP-UHFFFAOYSA-N
一般描述
一种吡咯烷氨基甲酸酯化合物,作为一种特定的REV-ERB-α/β激动剂。表现出直接和可逆的结合(Kd = 800 nM REV-ERB-α),并且与46个其他核受体相比表现出优异的选择性。显著增加REV-ERB依赖性阻遏物活性(Gal4 REV-ERB-α和β转染的HEK 293细胞的IC50分别为670和800 nM),并降低HepG2细胞的BMAL1 mRNA(IC50 = 710 nM)。显示穿过血脑屏障,并表现出理想的药代动力学特性。SR9009(100 mg/kg, i.p., b.i.d.)7天给药,可使C57BL6小鼠体重和脂肪显著下降,同时降低血糖和游离脂肪酸水平,并改变昼夜节律模式。
生化/生理作用
主靶
REV-ERB-α/&β
REV-ERB-α/&β
可逆性:是
细胞可渗透性:是
包装
用惰性气体包装
警告
毒性:标准处理(A)
重悬
复溶后,等分并冷冻保存(-20°C)。贮备溶液在-20°C下可稳定保存至多6个月。
其他说明
Solt, L.A., et al. 2012.Nature485, 62.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
10 - Combustible liquids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
iScience, 24(10), 103144-103144 (2021-09-22)
The coronavirus disease 2019 pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) coronavirus, is a global health issue with unprecedented challenges for public health. SARS-CoV-2 primarily infects cells of the respiratory tract via spike glycoprotein binding to angiotensin-converting
Cellular and molecular gastroenterology and hepatology, 12(2), 395-425 (2021-03-07)
Rev-erbα represents a powerful transcriptional repressor involved in immunity. However, the regulation, function, and clinical relevance of Rev-erbα in Helicobacter pylori infection are presently unknown. Rev-erbα was examined in gastric samples from H pylori-infected patients and mice. Gastric epithelial cells (GECs)
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