This is a demo store. No orders will be fulfilled.

CP-346086

    级别和纯度:
  • ≥99%
有货

库存信息

关闭

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
C649049-5mg
5mg 期货 Stock Image
C649049-10mg
10mg 期货 Stock Image

基本描述

规格或纯度 ≥99%
英文名称 CP-346086
生化机理 CP-346086 是一种强效口服活性微粒体甘油三酯转移蛋白(MTP)抑制剂,对人类和啮齿类动物 MTP 的 IC 50 为 2.0 nM。CP-346086 可降低体内血浆胆固醇和甘油三酯。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


CP-346086 is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC 50 of 2.0 nM for human and rodent MTP. CP-346086 can lower plasma cholesterol and triglycerides in vivo

In Vitro

CP-346086 (0.1-1000 nM) dose-dependently inhibits human MTP-mediated triglyceride transfer between vesicles with an IC 50 of 2.0 nM. CP-346086 (24 h) inhibits apolipoprotein B (apoB) and triglyceride secretion (IC 50 =2.6 nM) from Hep-G2 cells without affecting apoA-I secretion or lipid synthesis. 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

Form:Solid

IC50& Target:IC50: 2.0 nM (MTP)

纯度 ≥99%

关联靶点(其它种属)

Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IIUPAC Name N-[2-(1H-1,2,4-triazol-5-ylmethyl)-3,4-dihydro-1H-isoquinolin-6-yl]-2-[4-(trifluoromethyl)phenyl]benzamide
INCHI 1S/C26H22F3N5O/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)
InChi Key WNDIAFXQKOHFLV-UHFFFAOYSA-N
Smiles C1CN(CC2=C1C=C(C=C2)NC(=O)C3=CC=CC=C3C4=CC=C(C=C4)C(F)(F)F)CC5=NC=NN5
Isomeric SMILES C1CN(CC2=C1C=C(C=C2)NC(=O)C3=CC=CC=C3C4=CC=C(C=C4)C(F)(F)F)CC5=NC=NN5
PubChem CID 9826309
分子量 477.5

化学和物理性质

溶解性 DMSO : 100 mg/mL (209.43 mM; Need ultrasonic)
分子量 477.500 g/mol
XLogP3 4.700
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 7
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 477.178 Da
单同位素质量Monoisotopic Mass 477.178 Da
拓扑极表面积Topological Polar Surface Area 73.900 Ų
重原子数Heavy Atom Count 35
形式电荷Formal Charge 0
复杂度Complexity 714.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器