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Product details

名称

Pactimibe sulfate

分子类型

小分子

别名

硫酸帕替米贝

英文别名

英文名称

Pactimibe sulfate

货号

P651174-5mg

包装规格

5mg

浓度

≥98%

储存温度

2-8°C储存,干燥

运输条件

冰袋运输

产品介绍

Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC 50 s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC 50 s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a K i value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC 50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity . In Vitro Pactimibe sulfate (CS-505) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Pactimibe sulfate (CS-505; 60 and 200 mg/kg/day; oral gavage; twice a day; 12 weeks) induces an inhibition for ACAT-1 and ACAT-2, causing a reduction of plasma cholesterol but no influence on macrophage- or collagen-positive areas. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J ApoE −/− mice aged 8-week-oldDosage: 60 and 200 mg/kg/day Administration: Oral gavage; twice a day; 12 weeks Result: Decreased plasma cholesterol levels by 39% and 74% at the administration of 60 and 200 mg/kg/day. Form:Solid IC50& Target:ACAT1|4.9 μM (IC|50|)|ACAT2|3.0 μM (IC|50|)|ACAT|2 μM (IC|50|, in the liver)|ACAT|2.7 μM (IC|50|, in macrophages)|ACAT|4.7 μM (IC|50|, in THP-1 cells)|oleoyl-CoA|5.6 μM (Ki)|cholesteryl ester formation|6.7 μM (IC|50|)

生化机理

硫酸帕替麦布（CS-505）是一种 ACAT1/2 双重抑制剂，其 IC 50 s 分别为 4.9 μM 和 3.0 μM。硫酸帕替麦布（CS-505）在肝脏、巨噬细胞和 THP-1 细胞中抑制 ACAT 的 IC 50 s 分别为 2.0 μM、2.7 μM、4.7 μM。帕替米贝

CAS号

608510-47-0

分子式

C25H40N2O3.1/2H2O4S

分子量

465.65 g/mol

PubChem编号

11953348

Isomeric SMILES

CCCCCCCCN1CCC2=C(C(=C(C(=C21)NC(=O)C(C)(C)C)C)CC(=O)O)C.CCCCCCCCN1CCC2=C(C(=C(C(=C21)NC(=O)C(C)(C)C)C)CC(=O)O)C.OS(=O)(=O)O

IIUPAC Name

2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindol-5-yl]acetic acid;sulfuric acid

INCHI

1S/2C25H40N2O3.H2O4S/c2*1-7-8-9-10-11-12-14-27-15-13-19-17(2)20(16-21(28)29)18(3)22(23(19)27)26-24(30)25(4,5)6;1-5(2,3)4/h2*7-16H2,1-6H3,(H,26,30)(H,28,29);(H2,1,2,3,4)

InChi Key

MKJQESRCXYYHFR-UHFFFAOYSA-N

Smiles

CCCCCCCCN1CCC2=C(C(=C(C(=C21)NC(=O)C(C)(C)C)C)CC(=O)O)C.CCCCCCCCN1CCC2=C(C(=C(C(=C21)NC(=O)C(C)(C)C)C)CC(=O)O)C.OS(=O)(=O)O

PubChem CID

11953348

关联CAS

608510-47-0

MeSH Entry Terms

(7-(2,2-dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl)acetic acid hemisulfate;CS-505;pactimibe;pactimibe sulfate

溶解性

DMSO : 120 mg/mL (257.70 mM; Need ultrasonic) H2O : <0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

930.575 Da

单同位素质量Monoisotopic Mass

930.575 Da

拓扑极表面积Topological Polar Surface Area

222.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

653.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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