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SKF 104976是一种32-羧酸衍生物，具有强效的14α-脱甲基酶（14 alpha DM）抑制活性。SKF 104976以2 nM的浓度在Hep G2细胞提取物中抑制14 alpha DM活性达50%。SKF 104976在相似浓度下处理完整细胞时，抑制了[14C]乙 acetate在胆固醇中的掺入，并伴随有lanosterol的积累，同时导致3-羟基-3-甲基戊二酰辅酶A还原酶（HMGR）活性降低40-70%。SKF 104976不会影响Hep G2细胞中低密度脂蛋白的摄取和降解，表明HMGR和低密度脂蛋白受体活性在这些条件下并未协调调节。即使在甾醇合成途径中碳单位的流量减少达80%时，SKF 104976对HMGR活性的抑制效果仍然未改变。在由lovastatin几乎完全阻断的甾醇合成条件下，SKF 104976并未抑制HMGR活性。

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SKF 104976 Chemical Structure

SKF 104976 Chemical Structure

CAS No. : 136209-43-3

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SKF 104976 相关抗体

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生物活性

SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin[1].

分子量

470.73

Formula

C31H50O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SKF 104976 相关分类

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Keywords:

SKF 104976136209-43-3SKF104976SKF-104976OthersInhibitorinhibitorinhibit

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