2. Metabolic Enzyme/Protease
  3. Farnesyl Transferase
  4. RPR107393

RPR107393 是一种口服有效的选择性角鲨烯合酶 (SQS) 抑制剂。RPR107393 抑制大鼠肝微粒体角鲨烯合酶，IC50 值为 0.8 nM。RPR107393 通过增加细胞内法呢醇及其衍生物来抑制脂肪酸的生物合成，从而降低甘油三酯的生物合成。RPR107393 可降低大鼠和狨猴的血浆胆固醇。RPR107393 可用于代谢性疾病的相关研究，例如高胆固醇血症、高甘油三酯血症和动脉粥样硬化。

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RPR107393

RPR107393 Chemical Structure

CAS No. : 190841-57-7

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Other Forms of RPR107393:

RPR107393 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RPR107393 is an orally active potent selective squalene synthase (SQS) inhibitor. RPR107393 inhibits rat liver microsomal squalene synthase with an IC50 value of 0.8 nM. RPR107393 reduces triglyceride biosynthesis by suppressing fatty acid biosynthesis via an increase in intracellular farnesol and its derivatives. RPR107393 reduces plasma cholesterol in rats and marmosets. RPR107393 can be used for metabolic disease research, such as hypercholesterolemia, hypertriglyceridemia and atherosclerosis[1][2].

IC50 & Target

IC50: 0.8±0.2 nM (rat liver microsomal squalene synthase)[1]
体外研究
(In Vitro)

RPR107393 (10 分钟) 是大鼠肝微粒体角鲨烯合酶的强效抑制剂，IC50 值为 0.6 至 0.9 nM，对大鼠肝微粒体中的 HMG-CoA 还原酶无活性 (1 mM 时抑制率为 3%)[1]。
RPR107393 (6 小时) 浓度依赖性地抑制大鼠肝细胞中的胆固醇生物合成 (IC50 = 880 nM) 和甘油三酯生物合成 (IC50 = 410 nM)[2]。
RPR107393 (10 μM，2-24 小时) 以大鼠肝细胞中 [1-14C] 乙酸掺入脂质的程度呈时间依赖性降低，其对胆固醇和甘油三酯生物合成的最大抑制作用分别出现在 2 小时和 24 小时[2]。
RPR107393 (1 μM，4 小时) 分别抑制大鼠肝细胞中胆固醇和甘油三酯的生物合成 82.4% 和 70.0%，后者效应可通过补充 MVL 增强，提示其作用机制可能与 FPP 衍生物增加有关[2]。
RPR107393 (1-10 μM，4 小时) 可增强肉碱依赖性线粒体 β- 氧化 (1 μM 时增加 26.5%，10 μM 时增加 39.5%)，并通过不依赖 β- 氧化的途径降低整体甘油三酯的生物合成[2]。
RPR107393 (10 μM，4 小时) 通过抑制脂肪酸合成 (而非后续代谢阶段)，使大鼠肝细胞中脂肪酸和甘油三酯的合成分别降低 67.7% 和 68.5%，从而抑制甘油三酯的生物合成[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RPR107393 相关抗体:
体内研究
(In Vivo)

RPR107393 (10、25 和 30 mg/kg， 口服， 单次给药，或一日两次持续 2-4 天，或一日一次持续 7 天) 在大鼠模型中发挥强效降脂作用[1]。
RPR107393 (20 mg/kg， 口服， 一日两次或一日一次，持续 7 天) 在狨猴模型中，能选择性降低低密度脂蛋白胆固醇，同时维持有益的高密度脂蛋白水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (130-150 g)[1]
Dosage: 10 and 25 mg/kg
Administration: p.o., sigle dose
Result: Reduced cholesterol biosynthesis by 92% at 10 mg/kg, with an approximate ED50 value of 5 mg/kg.
Reduced cholesterol biosynthesis by 74 % after 6 h, and the time for 50% inhibition was ~7 hr at 10 mg/kg.
Inhibited hepatic cholesterol biosynthesis with an inhibition of 82% at 25 mg/kg after 10 h, but the effect was no longer apparent at 21 h.
Inhibited cholesterol biosynthesis associated with an accumulation of radiolabeled diacid products in the liver.
Animal Model: Sprague-Dawley rats (130-150 g)[1]
Dosage: 30 mg/kg
Administration: p.o., b.i.d. for 2-4 days
Result: Lowered serum cholesterol by 35% after 2 days and by nearly 50% after 3 days.
The reduction in cholesterol was greater in the very low-density lipoprotein (VLDL) and low-density lipoprotein (LDL) fractions (66-88%) than in the high-density lipoprotein (HDL) fraction (maximum, 35%).
Reduced serum triglycerides by up to 70%.
Induced hepatic microsomal HMG-CoA reductase activity by 12 to 34-fold.
Animal Model: Sprague-Dawley rats (130-150 g) given a chow diet or the same diet supplemented with 2 % cholestyramine (HY-104081)[1]
Dosage: 30 mg/kg
Administration: p.o., q.d. for 7 days
Result: The R and S enantiomers reduced serum cholesterol by 9% and 24%, and triglycerides by 46% and 57%, respectively.
Coadministration with 2% cholestyramine in the diet reduced serum cholesterol by 49%.
The R enantiomer administered alone did not lower serum LDL cholesterol, whereas coadministration with cholestyramine resulted in a 30% reduction.
The reductions in LDL cholesterol with the S enantiomer in the absence and the presence of cholestyramine were 33% and 61%, respectively.
The reduction was greater in the VLDL and LDL fractions than in the HDL fraction.
Animal Model: Male common marmosets (Callithrix jacchus)[1]
Dosage: 20 mg/kg
Administration: p.o., b.i.d. for 7 days
Result: Reduced plasma cholesterol by 50%.
The reduction in plasma cholesterol was selectively in the LDL fraction (≤50%), whereas cholesterol in the HDL fraction was unchanged.
Produced a greater reduction in plasma cholesterol than Lovastatin (HY-N0504) or Pravastatin (HY-B0165) (which produced ≤31% reduction at 50 mg/kg, b.i.d.).
Animal Model: Male common marmosets (Callithrix jacchus)[1]
Dosage: 20 mg/kg
Administration: p.o., q.d. for 7 days
Result: Both enantiomers reduced total plasma cholesterol by approximately 27%.
The R and S enantiomers reduced LDL cholesterol by 50% and 43%, respectively.
Showed no significant changed in HDL cholesterol levels.
分子量

403.34

Formula

C22H24Cl2N2O
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

RPR107393 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RPR107393190841-57-7RPR 107393RPR-107393Farnesyl TransferaseFtasesqualene synthaseSQSrat liver microsomaltriglyceride biosynthesisfarnesolratmarmosethypercholesterolemiahypertriglyceridemiaatherosclerosisInhibitorinhibitorinhibit

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