货号:A183954
同义名:
REV-ERB Agonist II
SR9009 is an agonist of REV-ERBα and REV-ERBβ with IC50 of 670 nM and 800 nM, respectively.
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描述 | The nuclear receptors REV-ERBα and -β link circadian rhythms and metabolism. SR-9009 is a potent synthetic REV-ERB agonist with IC50 value of 710nM for suppression of transcription in a cotransfection assay using full-length REV-ERB-a along with a luciferase reporter driven by the Bmal1 promoter. Administration of SR-9009 at dose of 100mg/kg, i.p., b.i.d., for 30 days resulted in a decrease in fat mass and in plasma lipids in diet-induced obese mice. SR9009 at concentration ranging in 2.5-20μM dose-dependently decreased mESC viability, rewired cellular metabolism shown by reduction of mitochondrial respiration, both of which were independent of REV-ERBs, and altered gene transcription in hepatocytes and embryonic stem cells lacking both REV-ERBα and –β, suggesting SR9009 may not be used solely as surrogate for REV-ERB activity. |
作用机制 | SR-9009 directly binds to REV-ERB-α.[1] |
Dose | Mice: 30 mg/kg - 100 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.28mL 0.46mL 0.23mL |
11.42mL 2.28mL 1.14mL |
22.83mL 4.57mL 2.28mL |
CAS号 | 1379686-30-2 |
分子式 | C20H24ClN3O4S |
分子量 | 437.94 |
SMILES Code | O=C(N1CC(CN(CC2=CC=C(Cl)C=C2)CC3=CC=C([N+]([O-])=O)S3)CC1)OCC |
MDL No. | N/A |
别名 | REV-ERB Agonist II |
运输 | 蓝冰 |
InChI Key | MMJJNHOIVCGAAP-UHFFFAOYSA-N |
Pubchem ID | 57394020 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 105 mg/mL(239.76 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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