<生产厂家价格>

SR12813

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。

SR12813名称

[ CAS 号 ]:
126411-39-0

[ 中文名 ]:
SR12813

[ 英文名 ]:
SR-12813

[英文别名 ]:

SRL
HTMT dimaleate
1ilh
BIDD:PXR0009
SR 12813

SR12813生物活性

[ 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.

[相关活性小分子]

SR12813物理化学性质

[ 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℃

SR12813安全信息

[ 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

SR12813文献

Dehydroepiandrosterone induces human CYP2B6 through the constitutive androstane receptor.

Drug Metab. Dispos. 35 , 1495-501, (2007)

Dehydroepiandrosterone (DHEA), the major precursor of androgens and estrogens, has several beneficial effects on the immune system, on memory function, and in modulating the effects of diabetes, obesi...

Cyclin-dependent kinase 2 negatively regulates human pregnane X receptor-mediated CYP3A4 gene expression in HepG2 liver carcinoma cells.

J. Biol. Chem. 283 , 30650-7, (2008)

The human pregnane X receptor (hPXR) regulates the expression of critical drug metabolism enzymes. One of such enzymes, cytochrome P450 3A4 (CYP3A4), plays critical roles in drug metabolism in hepatoc...

Isolation of mutant cells lacking Insig-1 through selection with SR-12813, an agent that stimulates degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase.

J. Biol. Chem. 279 , 43136-47, (2004)

Insig-1 and Insig-2 are membrane proteins of the endoplasmic reticulum that regulate lipid metabolism by the following two actions: 1) sterol-induced binding to 3-hydroxy-3-methylglutaryl-coenzyme A r...

更多文献