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编 号：F102819
分子式：C26H26F3N5O3
分子量：513.51
分子式：C26H26F3N5O3
分子量：513.51
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CAS No: 1262769-98-1
产品详情
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.
体内研究：
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.Animal Model:B6CBAF1J mice
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.
体外研究：
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.
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.
体内研究：
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.Animal Model:B6CBAF1J mice
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.
体外研究：
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.
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