SR12813

更新时间：2024-01-02 18:08:24

SR12813结构式	常用名	SR12813	英文名	SR-12813
	CAS号	126411-39-0	分子量	504.53400
	密度	1.117g/cm3	沸点	552.6ºC at 760mmHg
	分子式	C₂₄H₄₂O₇P₂	熔点	N/A
	MSDS	美版	闪点	288ºC

SR12813用途

SR12813 是有效的3-羟基-3-甲基-戊二酰辅酶A还原酶 (HMG-CoA reductase) 抑制剂,IC50 值为 0.85 μM。

中文名	SR12813
英文名	sr12813
英文别名	更多

描述	SR12813 是有效的3-羟基-3-甲基-戊二酰辅酶A还原酶 (HMG-CoA reductase) 抑制剂,IC50 值为 0.85 μM。
相关类别	信号通路 >> 代谢酶/蛋白酶 >> HMG-CoA还原酶(HMGCR) 研究领域 >> 代谢疾病
靶点	IC50: 0.85 μM (HMG-CoA Reductase)
体外研究	SR-12813抑制氚化水掺入胆固醇,IC50为1.2μM,但对脂肪酸合成没有影响。此外,SR-12813还能降低细胞3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶活性,IC50为0.85μM[1]。 25-HC和SR-12813都可以通过阻断胆固醇的合成来杀死哺乳动物细胞,因此它们是致命选择的理想试剂。 SR-12813在8μM至16μM的浓度范围内杀死HeLa细胞。 SR-12813杀死由Ad-Cre(SL-5 + Cre)感染的野生型细胞和突变细胞,但突变体SL-5在这种情况下存活。 SR-12813或25-HC促进野生型HeLa和SL-5突变细胞中95-KDa全长HMG-CoA还原酶的降解[1]。
激酶实验	简而言之，将化合物以Me 2 SO（最终浓度，0.1％）加入细胞中。在实验后，通过在室温下加入0.1mL 0.25％Brij 96,0.1M蔗糖，0.1M KF，50mM KCl，40mM二氢磷酸钾，30mM EDTA，5mM二硫苏糖醇，pH 7.4来裂解细胞。在一些实验中，省略KF以测量“总”HMG-CoA还原酶活性。进一步测定细胞裂解物中的HMG-CoA还原酶活性。
参考文献	[1]. Berkhout T, et al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J Biol Chem. 1996 Jun 14;271(24):14376-82. [2]. Jiang W, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632.

密度	1.117g/cm3
沸点	552.6ºC at 760mmHg
分子式	C₂₄H₄₂O₇P₂
分子量	504.53400
闪点	288ºC
精确质量	504.24100
PSA	110.91000
LogP	7.81780
外观性状	粉末
蒸汽压	8.02E-13mmHg at 25°C
折射率	1.504
储存条件	-20℃

个人防护装备	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
危险品运输编码	NONH for all modes of transport

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SR 12813