阿伐麦布
货号：
IA4640
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| MDL | MFCD00934956 |
| EC | EINECS 1592732-453-0 |
| 别名 | PD-14851 |
| 英文名称 | Avasimibe |
| CAS | 166518-60-1 |
| 分子式 | C29H43NO4S |
| 分子量 | 501.72 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | White to off-white Powder |
| 单位 | 瓶 |
| 生物活性 | vasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 μM for ACAT1 and ACAT2, respectively[1]. Avasimibe can be used for the research of prostate cancer[2]. |
| In Vitro | Avasimibe (0, 0.25, 5, 10, 20, 40 and 80 μM; for 1, 2, and 3 days) reduces proliferation in the prostate cancer (PCa) cells.Avasimibe (10 and 20 μM; 48 h) reduces the expression of β-catenin, Vimentin, N-cadherin, Snail and MMP9, which are tightly associated with epithelial-mesenchymal transition (EMT).Avasimibe (10 and 20 μM) trigger cell cycle arrest via the E2F-1 signalling pathway in prostate cancer. Avasimibe induces G1 phase cell cycle arrest of PCa cells.Avasimibe (10 and 20 μM) inhibits the metastasis of PCa cells[2]. |
| In Vivo | Avasimibe (30 mg/kg, intraperitoneally injected on alternate days for 7 weeks) suppresses PCa cell growth and metastasis in vivo. Avasimibe has good biocompatibility and low toxicity[2]. |
| SMILES | O=C(NS(=O)(OC1=C(C(C)C)C=CC=C1C(C)C)=O)CC2=C(C(C)C)C=C(C(C)C)C=C2C(C)C |
| 靶点 | cholesterol acyltransferase (ACAT)，CYP2C9/ CYP1A2/CYP2C19 |
| 数据来源文献 | [1]. Taichi Ohshiro,et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15. [2]. Kangping Xiong, et al. The cholesterol esterification inhibitor avasimibe suppresses tumour proliferation and metastasis via the E2F-1 signalling pathway in prostate cancer.Cancer Cell Int. 2021 Aug 30;21(1):461. |
| 规格 | 5mg 10mg |
Avasimibe抑制ACAT，也抑制人P450同工酶CYP2C9， CYP1A2和CYP2C19。