1. Metabolic Enzyme/Protease
  2. Microsomal Triglyceride Transfer Protein (MTP)
  3. CP-346086 dihydrate

CP-346086 dihydrate 是一种有效和具有口服活性的微粒体甘油三酯转移蛋白 (MTP) 抑制剂,对人和啮齿动物 MTP 的 IC50 为 2.0 nM。CP-346086 dihydrate 可在体内降低血浆胆固醇和甘油三酯。

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CP-346086 dihydrate Chemical Structure

CP-346086 dihydrate Chemical Structure

CAS No. : 1262769-98-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CP-346086 dihydrate is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 dihydrate can lower plasma cholesterol and triglycerides in vivo[1].

IC50 & Target

IC50: 2.0 nM (MTP)[1]

体外研究
(In Vitro)

CP-346086 (0.1-1000 nM) dose-dependently inhibits human MTP-mediated triglyceride transfer between vesicles with an IC50 of 2.0 nM[1].
CP-346086 (24 h) inhibits apolipoprotein B (apoB) and triglyceride secretion (IC50=2.6 nM) from Hep-G2 cells without affecting apoA-I secretion or lipid synthesis[1].

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

体内研究
(In Vivo)

CP-346086 (1-100 mg/kg; oral gavage once daily for 2 weeks) reduces plasma total, VLDL, and LDL cholesterol and triglycerides in mice[1].
CP-346086 (25 mg/kg; a single p.o.) results in an almost complete inhibition of Tyloxapol-induced triglyceride accumulation in fasted rats[1].
CP-346086 (0.1-10 mg/kg; a single p.o.) reduces acute plasma triglyceride in mice[1].

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

Animal Model: B6CBAF1J mice[1]
Dosage: 1, 2, 10, 20, 100 mg/kg
Administration: Oral gavage once daily for 2 weeks
Result: Lowered total, VLDL, and LDL cholesterol and triglycerides dose dependently with 23%, 33%, 75%, and 62% reductions at 10 mg/kg/day.
分子量

513.51

Formula

C26H26F3N5O3

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
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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • 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.

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CP-346086 dihydrate
目录号:
HY-113955A
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