SML2067
SR9011
≥98% (HPLC), nuclear receptor REV-ERB agonist, powder
别名:
3-[[[（4-氯苯基）甲基] [（5-硝基-2-噻吩基）甲基] 氨基] 甲基]-N-戊基-1-吡咯烷甲酰胺
产品名称
SR9011, ≥98% (HPLC)
color
white to beige
SMILES string
[s]1c(ccc1CN(CC3CN(CC3)C(=O)NCCCCC)Cc2ccc(cc2)Cl)[N+](=O)[O-]
InChI key
PPUYOYQTTWJTIU-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Application
Sr9011已用作核受体亚家族1 D组成员1(NR1D1)受体激动剂：
- 研究其对小胶质细胞免疫代谢的影响
- 研究其对人2型糖尿病胰岛细胞胰岛素分泌的影响
- 研究其对甲状腺刺激激素β (TSHβ)基因表达的影响
Biochem/physiol Actions
REV-ERB 激动剂是一种强效核受体 REV-ERB 激动剂（根据基于细胞的报告基因分析，REV-ERBα -和 REV-ERBβ-的 EC50依赖性阻遏蛋白活性分别 = 790 和 560 nM）在体外培养物和小鼠体内 (100 mg/kg i.p.，b.i.d.) 刺激 REV-ERB 依赖性靶基因抑制，而对一组 46 个其他核受体无活性。SR9011 通过抑制转录因子 BMAL1（脑和肌肉 ARNT 样蛋白 1）和 CLOCK（昼夜节律与细胞周期）调节昼夜节律行为，并通过调节小鼠体内脂肪和葡萄糖代谢相关基因诱导能量消耗和体重减轻，具有良好的生物利用度（血浆浓度）。分别为 0.53 和 15.3μ10 或 100 mg/kg i.p. 给药后 2 h；脑浓度= 0.24 μM 10 mg/kg i.p. 给药后 2 h），而其结构类似物 GSK4112 未显示血浆暴露。
修订版-ERBα/β培养物和小鼠体内促进 REV-ERB-依赖性抑制物活性的激动剂。
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
监管及禁止进口产品
此项目有
Sadichha Sitaula et al.
Biochemical pharmacology, 131, 68-77 (2017-02-19)
REV-ERBα and REV-ERBβ are heme regulated nuclear receptors that are known to regulate metabolic pathways. We previously demonstrated that treatment of mice with synthetic REV-ERB agonists suppressed plasma cholesterol levels and the hepatic levels of the rate limiting enzyme in
Irene O Aninye et al.
The Journal of biological chemistry, 289(24), 17070-17077 (2014-05-06)
Thyroid hormones (TH) are critical for development, growth, and metabolism. Circulating TH levels are tightly regulated by thyroid-stimulating hormone (TSH) secretion within the hypothalamic-pituitary-thyroid axis. Although circadian TSH secretion has been well documented, the mechanism of this observation remains unclear.
Laura A Solt et al.
Nature, 485(7396), 62-68 (2012-03-31)
Synchronizing rhythms of behaviour and metabolic processes is important for cardiovascular health and preventing metabolic diseases. The nuclear receptors REV-ERB-α and REV-ERB-β have an integral role in regulating the expression of core clock proteins driving rhythms in activity and metabolism.
Volodymyr Petrenko et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(5), 2484-2495 (2020-01-23)
Circadian clocks operative in pancreatic islets participate in the regulation of insulin secretion in humans and, if compromised, in the development of type 2 diabetes (T2D) in rodents. Here we demonstrate that human islet α- and β-cells that bear attenuated
Ryota Nakazato et al.
Glia, 65(1), 198-208 (2016-10-12)
Similar to neurons, microglia have an intrinsic molecular clock. The master clock oscillator Bmal1 modulates interleukin-6 upregulation in microglial cells exposed to lipopolysaccharide. Bmal1 can play a role in microglial inflammatory responses. We previously demonstrated that gliotransmitter ATP induces transient
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