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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to tan
溶解性
DMSO: ≥40 mg/mL
相关疾病
Alzheimer′s disease; cardiovascular diseases
储存温度
room temp
SMILES字符串
CC(C)c1cc(C(C)C)c(CC(=O)NS(=O)(=O)Oc2c(cccc2C(C)C)C(C)C)c(c1)C(C)C
InChI
1S/C29H43NO4S/c1-17(2)22-14-25(20(7)8)27(26(15-22)21(9)10)16-28(31)30-35(32,33)34-29-23(18(3)4)12-11-13-24(29)19(5)6/h11-15,17-21H,16H2,1-10H3,(H,30,31)
InChI key
PTQXTEKSNBVPQJ-UHFFFAOYSA-N
应用
阿伐麦布已被用作Huh7.5.1细胞中酰基辅酶A:胆固醇酰基转移酶(ACAT)的抑制剂,以测试其与直接作用抗病毒药物(DAA)的组合效果,以及其对适应酸中毒的癌细胞中脂质滴积累的影响。它可以用作ACAT的抑制剂来评估克氏锥虫中胆固醇的酯化。
生化/生理作用
阿伐麦布(CI-1011)是一种口服生物可利用的Acyl-CoA:胆固醇O-酰基转移酶(ACAT)抑制剂
阿伐麦布(CI-1011)是一种口服生物可利用的Acyl-CoA:胆固醇O-酰基转移酶(ACAT)抑制剂。它最初作为一种抗惊厥药物被开发,并且被证明能够显著降低血浆总甘油三酯和VLDL-胆固醇,但后来的临床试验令人失望。ACAT也被作为阿尔茨海默病的潜在治疗靶点进行了研究。最近已经研究了阿伐麦布通过限制可扩散淀粉样蛋白-β(Abeta)的产生和增加清除来削弱淀粉样蛋白病变的作用。
法律信息
根据辉瑞公司的协议出售,用于研究目的。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
[Acyl-coenzyme A: cholesterol acyltransferase (ACAT)].
Akira Miyazaki et al.
Nihon rinsho. Japanese journal of clinical medicine, 62 Suppl 12, 89-91 (2005-01-22)
Miria Gomes Pereira et al.
PloS one, 10(6), e0128949-e0128949 (2015-06-13)
Trypanosoma cruzi epimastigotes store high amounts of cholesterol and cholesteryl esters in reservosomes. These unique organelles are responsible for cellular digestion by providing substrates for homeostasis and parasite differentiation. Here we demonstrate that under nutritional lipid stress, epimastigotes preferentially mobilized
Jean-Claude Tardif et al.
The American journal of cardiology, 98(1), 23-27 (2006-06-21)
We assessed vascular changes during atherosclerosis regression. Compensatory enlargement of coronary arteries accommodates plaque burden during atherosclerosis development. Lipid-lowering therapy has altered the natural history of coronary atherosclerosis, but the arterial changes that occur during disease regression need to be
John R Burnett et al.
Biochimica et biophysica acta, 1738(1-3), 10-18 (2006-01-24)
Previously, we have shown, in vivo, that the acyl coenzyme A: cholesterol acyltransferase (ACAT) inhibitor avasimibe decreases hepatic apolipoprotein (apo) B secretion into plasma. To test the hypothesis that avasimibe modulates postprandial triglyceride-rich lipoprotein (TRL) metabolism in vivo, an oral
Yves Rival et al.
DNA and cell biology, 23(5), 283-292 (2004-06-01)
It is now recognized that atherosclerosis complications are related to the unstable character of the plaque rather than its volume. Vulnerable plaques often contain a large lipid core, a reduced content of smooth muscle cells, and accumulation of inflammatory cells.
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