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

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.

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CP-346086 dihydrate Chemical Structure

CP-346086 dihydrate Chemical Structure

CAS No. : 1262769-98-1

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Description

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]

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].

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

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].

MedChemExpress (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.
Molecular Weight

513.51

Formula

C26H26F3N5O3

CAS No.
SMILES

O=C(C1=CC=CC=C1C2=CC=C(C(F)(F)F)C=C2)NC3=CC4=C(CN(CC5=NC=NN5)CC4)C=C3.[H]O[H].[H]O[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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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Product Name:
CP-346086 dihydrate
Cat. No.:
HY-113955A
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