Avasimibe (Synonyms: 阿伐麦布; CI-1011; PD-148515)
目录号: PL14727 纯度: ≥99%
CAS No. :166518-60-1
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中文名称
Avasimibe
中文别名
阿伐麦布;N-(2,6-二异丙基苯氧基)磺酰-2-(2,4,6-三异丙基苯基)乙酰胺;Avasimibe 抑制剂;L-艾杜糖醛酸;AVASIMIBE 阿伐麦布;阿伐麦布溶液, 100PPM;AVASIMIBE;PD 148515
英文名称
Avasimibe
英文别名
2,6-Diisopropylphenyl (2-(2,4,6-triisopropylphenyl)acetyl)sulfamate;N-(2,6-Dipropan-2-ylphenoxy)sulfonyl-2-(2,4,6-tripropan-2-ylphenyl)acetamide;Avasimibe;[[2,4,6-tris(1-methylethyl)phenyl]acetyl]-, 2,6-bis(1-methylethyl)phenyl ester] sulfamic acid;2,6-Diisopropylphenyl (2-(2,4,6-triisopropylphenyl)-acetyl)sulfamate;AVASIMIBE(CI-1011);[2,6-di(propan-2-yl)phenyl] N-[2-[2,4,6-tri(propan-2-yl)phenyl]acetyl]sulfamate;CI1011;CI-1011;PD148515;PD-148515;Avasimibe Solution, 100ppm;2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate;N-[(2,6-DIISOPROPYLPHENOXY)SULFONYL]-2-(2,4,6-TRIISOPROPYLPHENYL)ACETAMIDE;((2,4,6-TRIS(1-METHYLETHYL)PHENYL)ACETYL)SULFAMICACID2,6-BIS(1-METHYLETHYL)PHENYLESTER;CI-1011; PD 148515; [[2,4,6-tris(1-methylethyl)phenyl]acetyl]-, 2,6-bis(1-methylethyl)phenyl ester] sulfamic acid;Avasimibe, >=98%;CI 1011;PD 148515;28LQ20T5RC;2,6-Diisopropylphenyl ((2,4,6-triisopropylphenyl)acetyl)sulfamate;((2,4,6-Tris(1-methylethyl)phenyl)acetyl)sulfamic acid 2,6-bis(1-methylethyl)phenyl ester;N;avasimibe;Avasimibe(CI-1011);n-(2,6-dipropan-2-ylphenoxy)sulfonyl-2-(2,4,6-tripropan-2-ylphenyl)acetamide
Cas No.
166518-60-1
分子式
C29H43NO4S
分子量
501.72
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Avasimibe (CI-1011; PD-148515) 是一种有效的,具有口服活性的酰基辅酶 A: 胆固醇酰基转移酶 (ACAT) 抑制剂,对 ACAT1 和 ACAT2 的 IC50 分别为 24 和 9.2 µM。Avasimibe 可用于前列腺癌的研究。
生物活性
Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC 50 s of 24 and 9.2 μM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
性状
Solid
IC50 & Target[1][2]
ACAT1 24 μM (IC50) ACAT2 9.2 μM (IC50
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (199.31 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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