Torcetrapib托彻普,262352-17-0

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Torcetrapib

CAS No. : 262352-17-0

MCE 国际站：Torcetrapib

产品活性：Torcetrapib (CP-529414) 是一种选择性、有效的胆固醇酯转移蛋白 (CETP) 抑制剂。 在人血浆的抑制曲线中对CETP的最有效浓度为 37 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：CETP

In Vitro: The IC₅₀ for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the ³H-HDL and ¹⁴C-LDL cholesteryl ester transfer assays, respectively, using the specific activity-adjusted calculation, and 47 and 61 nM using a single exponential decay function.
Torcetrapib (0, 0.5, 1, 5, and 10 μM) significantly reduced MCF-7 cells growth.
Torcetrapib (0, 1, 5, 10, and 20 μM) does not inducing MCF-7 cells apoptosis.
Torcetrapib (10 μM) binds to CETP with high affinity and down-regulates CETP expression.

In Vivo: Torcetrapib (3, 10, or 30 mg/kg every day [qd]; oral gavage for 14 days) significantly increases high-density lipoprotein (HDL) cholesterol and reduceslow-density lipoprotein (LDL) cholesterol, and there is a tendency for Torcetrapib to reduce very-low-density lipoprotein (VLDL) cholesterol and triglycerides. Maximal increase in HDL cholesterol is 53% with Torcetrapib.

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