| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S407772-1ml |
1ml |
现货  |
|
| 英文别名 | MK-0733 | 2,2-dimethyl-butanoic acid-(1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl ester |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Simvastatin (MK 733) |
| 生化机理 | 辛伐他汀（MK-0733，MK 733）是 HMG-CoA 还原酶的竞争性抑制剂，在无细胞试验中的Ki值为 0.1-0.2 nM。辛伐他汀可诱导铁变态反应、有丝分裂、自噬和细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | HMG-CoA 还原酶抑制剂 |
| 产品介绍 |
辛伐他汀是药物前体。辛伐他汀是洛伐他汀的半合成衍生物/类似物。辛伐他汀不溶于水，但可溶于极性有机溶剂。 产品用途： 辛伐他汀已用于： Information Simvastatin (MK 733) Simvastatin (MK-0733, MK 733) is a competitive inhibitor of HMG-CoA reductase with K i of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis , mitophagy , autophagy and apoptosis . Prior to use in cell assays, Simvastatin needs to be activated by NaOH in EtOH treatment. Simvastatin inhibits cholesterol synthesis in mouse L-M cell (fibroblast), rat H4II E cell (liver), and human Hep G2 cell (liver) with IC50 of 19.3 nM, 13.3 nM and 15.6 nM, respectively. Simvastatin treatment leads to 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 displays anti-inflammatory effects in vitro. Simvastatin (10 μM) 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. Simvastatin (10 μM) suppresses cell-mediated macrophage TNF-γ release induced via cognate interactions by ~30%. In vivo Simvastatin orally administration inhibits the conversion of radiolabeled acetate to cholesterol with IC50 of 0.2 mg/kg. Simvastatin (4 mg/day) orally administration for 13 weeks to rabbits fed an atherogenci cholesterol-rich diet, returns the cholesterol-induced increases in total cholesterol, LDL-cholesterol and HDL-cholesterol to normal level. Simvastatin (6 mg/kg) produces an increase in LDL receptor-dependent binding and increases the number of hepatic LDL receptors in rabbits fed a diet containing 0.25% cholesterol. Simvastatin influences inflammation independent of its effect on plasma cholesterol level. In cynomolgus monkeys consumed an atherogenic diet, Simvastatin (20 mg/kg/day) induces 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. cell lines： Concentrations： Incubation Time： Powder Purity:≥95% |
| ALogP | 4.7 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CCC(C)(C)C(=O)O[C@H]1C[C@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@@H]3C[C@H](CC(=O)O3)O)C |
| PubChem CID | 54454 |
| 分子量 | 418.57 |
| Reaxy-Rn | 4768037 |
| 溶解性 | Solubility (25°C) In vitro |
|---|---|
| 比旋光度 | 293° (C=1,CH3CN) |
| 熔点 | 134°C |
| 象形图 | GHS09, GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
H315: 引起皮肤刺激 H410: 对水生生物有剧毒并具有长期持续影响 H362: 可能对母乳喂养的孩子造成伤害 |
| 预防措施声明 |
P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。 P391: 收集溢出物 P263: 避免在怀孕期间/哺乳期间接触。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。 P332+P317: 如果出现皮肤刺激：请寻求医疗帮助。 |
| WGK Germany | 2 |
| RTECS | EK7798000 |
| Merck Index | 8539 |
| 个人防护装备 | Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter |
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