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抑制剂/激活剂

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凋亡与自噬

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Simvastatin 辛伐他汀; MK 733

Simvastatin是一种HMG-CoA reductase竞争性抑制剂，无细胞试验中Ki为0.1-0.2 nM。Simvastatin可诱导铁死亡、线粒体自噬、细胞自噬和凋亡。

货号：
TK0204
规格：

2mg

5mg

10mg

50mg

100mg
价格：
￥0.00

产品参数

CAS No.	79902-63-9
生物活性	Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
分子式	C25H38O5
分子量	418.57
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	Ethanol : 100 mg/mL (238.91 mM; Need ultrasonic) DMSO : ≥ 50 mg/mL (119.45 mM)
体内研究	Simvastatin suppresses the conversion of radiolabeled acetate to cholesterol with an IC50 of 0.2 mg/kg via p.o. administration. Simvastatin (4 mg/day, p.o. for 13 weeks) returns the cholesterol-induced increases in total cholesterol, LDL-cholesterol and HDL-cholesterol to normal level in rabbits fed an atherogenci cholesterol-rich diet. Simvastatin (6 mg/kg) increases LDL receptor-dependent binding and the number of hepatic LDL receptors in rabbits fed a diet containing 0.25% cholesterol. Simvastatin affects inflammation independent of its effect on plasma cholesterol level. Simvastatin (20 mg/kg/day) causes a 1.3-fold less macrophage content in lesions, and 2-fold less vascular cell adhesion molecule-1, interleukin-1beta, and tissue factor expression, companied by a 2.1-fold increases in lesional smooth muscle cell and collagen content in cynomolgus monkeys fed an atherogenic diet.
体外研究	Simvastatin needs to be activated by NaOH in EtOH treatment before use for cell assay (Activation of Simvastatin: 2 mg of Simvastatin in 50 μL of ethanol and 75 μL of 0.1 N NaOH, incubated at 50°C for 2 hours. The pH is adjusted to 7.2 with HCl). Simvastatin suppresses cholesterol synthesis in mouse L-M cell, rat H4II E cell, and human Hep G2 cell with IC50s of 19.3 nM, 13.3 nM and 15.6 nM, respectively. Simvastatin causes a dose-dependent increase in serine 473 phosphorylation of Akt within 30 minutes, with maximal phosphorylation occurring at 1.0 µM. Simvastatin (1.0 μM) enhances phosphorylation of the endogenous Akt substrate endothelial nitric oxide synthase (eNOS), inhibits serum-free media undergo apoptosis and accelerates vascular structure formation. Simvastatin shows anti-inﬂammatory effects, reduces anti-CD3/anti-CD28 antibody-stimulated proliferation of PB-derived mononuclear cells and synovial ﬂuid cells from rheumatoid arthritis blood, as well as IFN-γ release at 10 μM. Simvastatin (10 μM) also blocks cell-mediated macrophage TNF-γ release induced via cognate interactions by appr 30%. Simvastatin (5 μM) significantly reduces the expression of ABCA1 in astrocytes and neuroblastoma cells, the expression of apolipoprotein E in astrocytes, and increases cyclin-dependent kinase 5 and glycogen synthase kinase 3β expression in SK-N-SH cells.Simvastatin has the ability to inhibit exosome release.
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纯度及产品资料	98%

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