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.
Product information
CAS Number: 1262769-98-1
Molecular Weight: 513.51
Formula: C26H26F3N5O3
Chemical Name: N-{2-[(4H-1, 2, 4-triazol-3-yl)methyl]-1, 2, 3, 4-tetrahydroisoquinolin-6-yl}-4'-(trifluoromethyl)-[1, 1'-biphenyl]-2-carboxamide dihydrate
Smiles: O.O.O=C(NC1=CC2CCN(CC3NC=NN=3)CC=2C=C1)C1=CC=CC=C1C1C=CC(=CC=1)C(F)(F)F
InChiKey: QCUKFGSPPGIYIX-UHFFFAOYSA-N
InChi: InChI=1S/C26H22F3N5O.2H2O/c27-26(28,29)20-8-5-17(6-9-20)22-3-1-2-4-23(22)25(35)32-21-10-7-19-14-34(12-11-18(19)13-21)15-24-30-16-31-33-24;;/h1-10,13,16H,11-12,14-15H2,(H,32,35)(H,30,31,33);2*1H2
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
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. CP-346086 (25 mg/kg; a single p.o.) results in an almost complete inhibition of Tyloxapol-induced triglyceride accumulation in fasted rats. CP-346086 (0.1-10 mg/kg; a single p.o.) reduces acute plasma triglyceride in mice.
Products are for research use only. Not for human use.
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