438185
洛伐他汀
Lovastatin, CAS 75330-75-5, is an anti-hypercholesterolemic agent that inhibits the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase.
别名:
洛伐他汀, 洛伐他汀，MK-803，L型钙通道阻滞剂IV
质量水平
描述
Merck USA index - 14, 5586
方案
≥95% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white to off-white
溶解性
ethanol: 25 mg/mL
DMSO: 50 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
O1[C@@H](C[C@H](CC1=O)O)CC[C@@H]2[C@H]3[C@H](C[C@H](C=C3C=C[C@@H]2C)C)OC(=O)[C@H](CC)C
InChI
1S/C24H36O5/c1-5-15(3)24(27)29-21-11-14(2)10-17-7-6-16(4)20(23(17)21)9-8-19-12-18(25)13-22(26)28-19/h6-7,10,14-16,18-21,23,25H,5,8-9,11-13H2,1-4H3/t14-,15-,16-,18+,19+,20-,21-,23-/m0/s1
InChI key
PCZOHLXUXFIOCF-BXMDZJJMSA-N
一般描述
一种抑制3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶活性的抗高胆固醇血症剂。已显示阻断一系列生物事件，包括：胰岛素在3T3-L1成纤维细胞和3T3-L1脂肪细胞中激活p21ras；p21ras的法尼基化，减少了可用于随后被生长因子（包括胰岛素）激活的细胞内Ras池；和N-ras-诱导的神经元分化。通过抑制蛋白酶体导致细胞周期停滞在G1期晚期。最近已显示在HIRcB细胞中通过胰岛素抑制对MAP激酶的刺激，并阻断THP-1衍生的巨噬细胞中I型SCR基因的转录。还通过PDGF阻断PDGF受体酪氨酸磷酸化和 MAP激酶活化。该产品需要激活才能用于细胞同步化研究和HMG-CoA研究的无细胞测定系统。
一种抗高胆固醇血症药和3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂，可阻断一系列生物事件，包括：胰岛素在3T3-L1成纤维细胞和3T3-L1脂肪细胞中激活p21ras，p21ras的法尼基化，减少了可用于随后被生长因子（包括胰岛素）激活的细胞内Ras池，以及N-Ras诱导的神经元分化。导致细胞周期阻滞于G1晚期。显示在HIRcB细胞中通过胰岛素抑制对MAP激酶的刺激，并阻断THP-1衍生的巨噬细胞中I型SCR基因的转录。还通过PDGF阻断PDGF受体酪氨酸磷酸化和 MAP激酶活化。该产品需要激活才能用于细胞同步化研究和HMG-CoA研究的无细胞测定系统。
生化/生理作用
主要靶标
3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶的活性
3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶的活性
产物不与ATP竞争。
可逆：否
细胞渗透性：否
制备说明
复溶后等分，用惰性气体冲洗并冷冻（-20°C）保存。贮备液（含高质量DMSO或乙醇）在-20°C下可稳定保存长达1个月。
其他说明
Rao, S., et al. 1999.Proc.Natl.Acad.Sci. USA96, 7197.
Carel, K., et al. 1996.J. Biol. Chem.271, 30625.
McGuire, T.F., et al. 1996.J. Biol. Chem. 271, 27402.
Umetani, N., et al. 1996.Biochim.Biophys.Acta1303, 199.
Xu, X.Q., et al. 1996.Arch.Biochem.Biophys.326, 233.
Reusch, J.E.-B., et al. 1995.J. Biol. Chem.270, 2036.
Jakobisiak, M., et al. 1991.Proc.Natl.Acad.Sci.USA88, 3628.
Keyomarsi, K., et al. 1991.Cancer Res.51, 3602.
Mendola, C.E., and Backer, J.M.1990.Cell Growth Differ.1, 499.
Carel, K., et al. 1996.J. Biol. Chem.271, 30625.
McGuire, T.F., et al. 1996.J. Biol. Chem. 271, 27402.
Umetani, N., et al. 1996.Biochim.Biophys.Acta1303, 199.
Xu, X.Q., et al. 1996.Arch.Biochem.Biophys.326, 233.
Reusch, J.E.-B., et al. 1995.J. Biol. Chem.270, 2036.
Jakobisiak, M., et al. 1991.Proc.Natl.Acad.Sci.USA88, 3628.
Keyomarsi, K., et al. 1991.Cancer Res.51, 3602.
Mendola, C.E., and Backer, J.M.1990.Cell Growth Differ.1, 499.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
毒性：致癌/致畸（D）
警示用语：
Warning
危险声明
危险分类
Carc. 2 - Repr. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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