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My CartCAS：75330-75-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 75330-75-5 |
| Name | Lovastatin |
| Molecular Formula | C24H36O5 |
| Molecular Weight | 404.54 |
| Solubility | Soluble in DMSO ≥4mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 616-212-7 |
| MDL | MFCD00072164 |
| SMILES | O=C([C@@H](C)CC)O[C@@H]1[C@@]([C@H]2CC[C@@H](OC3=O)C[C@H](C3)O)([H])C(C=C[C@@H]2C)=C[C@H](C)C1 |
| InChIKey | PCZOHLXUXFIOCF-BXMDZJJMSA-N |
| InChI | 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 |
| PubChem CID | 53232 |
| Target Point | HMG-CoA Reductase (HMGCR) |
| Passage | Metabolic Enzyme&Protease |
| Background | Lovastatin is a cell-permeable HMG-CoA reductase inhibitor for cholesterol reduction. |
| Biological Activity | Lovastatin是一种用于降低胆固醇的细胞渗透性的 HMG-CoA还原酶抑制剂。[1-4] |
| In Vitro | 洛伐他汀是无活性的内酯前药，必须通过化学或酶促转化为其二羟基开环酸形式，以引发抑制活性。羟基酸形式的洛伐他汀是一种特别有效的肝HMG CoA还原酶竞争性抑制剂[1]。洛伐他汀除抗其抗胆固醇外，在骨质疏松症，神经变性，类风湿性关节炎，抗真菌药等领域具有多种应用，据报道还可减少肺癌细胞，乳腺癌(MCF-7)，肝癌(HepG2)的增殖。 。洛伐他汀治疗对HeLa细胞显示出显著的剂量依赖性细胞毒作用，IC50值为160μg/ mL。洛伐他汀可有效加速羟自由基清除活性(54.06％)，IC50为3601μg/ mL [2]。 |
| In Vivo | 洛伐他汀是一种无活性的内酯，在肝脏中水解成活性的f3-羟基酸形式。该主要代谢物是酶HMG-CoA还原酶的抑制剂。 Ki为1 nM。洛伐他汀及其β-羟基酸代谢物与人血浆蛋白高度结合。洛伐他汀穿过血脑和胎盘屏障[3]。洛伐他汀可显著降低含载脂蛋白B的脂蛋白，尤其是低密度脂蛋白胆固醇，血浆甘油三酯含量较低，高密度脂蛋白胆固醇含量略有增加[4]。 |
| Cell Experiment | 用洛伐他汀(0，5，10，20，40，80，160，320μg/ mL)处理Hela细胞24小时。用培养基处理的细胞用作阴性对照。使用基于MTT的比色测定法测量细胞活力[2]。 |
| Data Literature Source | [1]. Alberts AW，et al. Discovery，biochemistry and biology of lovastatin. Am J Cardiol. 1988 Nov 11;62(15):10J-15J. [2]. Bhargavi S，et al. Purification of Lovastatin from Aspergillus terreus (KM017963) and Evaluation of its Anticancer and Antioxidant Properties. Asian Pac J Cancer Prev. 2016;17(8):3797-803. [3]. Frishman WH，et al. Lovastatin: an HMG-CoA reductase inhibitor for lowering cholesterol. Med Clin North Am. 1989 Mar;73(2):437-48. [4]. Tobert JA，et al. Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26. |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 50mg |
是一种用于降低胆固醇的细胞渗透性的 HMG-CoA还原酶抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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