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Pyripyropene A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pyripyropene A图片
CAS NO:147444-03-9
包装:250 μg
市场价:4900元

产品介绍
Pyripyropene A 是一种高效、选择性的SOAT2/ACAT2抑制剂,其IC50值为 0.07 μM。Pyripyropene A 在体内能减轻高胆固醇血症和动脉粥样硬化。
生物活性

Pyripyropene A is a potent and selectivesterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterolacyltransferase2 (ACAT2)inhibitor, with anIC50of 0.07 μM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo[1][2][3][4].

IC50& Target

IC50: 0.07 μM (ACAT2)[1]

体外研究
(In Vitro)

Pyripyropene A (0-100 μM; 72 hours) exhibits anti-proliferative activity against HUVECs, and with an IC50value of 1.8 μM[1].
Pyripyropene A (10 μM ; 24 hours) inhibits VEGF (20 ng/ml)-induced migration and tubular formation of HUVECs in dose-dependent fashion[1].
Pyripyropene A do not show growth inhibitory effects against KB3-1, K562 and Neuro2A cells[1].

Cell Proliferation Assay[1]

Cell Line:HUVECs
Concentration:0-100 μM
Incubation Time:72 hours
Result:Exhibited anti-proliferative activity against HUVECs with an IC50value of 1.8 μM.
体内研究
(In Vivo)

Pyripyropene A (10-50 mg/kg per day; p.o; 12 weeks) reduces the levels of plasma cholesterol, very-low-density lipoprotein (VLDL), and low-density lipoprotein (LDL) and hepatic cholesterol content in apolipoprotein E-knockout mice. And Pyripyropene A-treated mice display reduction of atherogenic lesion areas in the aortae and heart[3].
Pyripyropene A inhibits the hepatic e acyl–coenzyme A:cholesterol acyltransferase 2 (ACAT2) activity in vivo[3].
Pyripyropene A displays a half-life (t1/2) of 0.693/λ, where λ represented the terminal slope of the log-linear portion of concentration time profile[4].

Animal Model:Male C57BL/6 mice[2]
Dosage:0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg
Administration:Oral administration; daily; for 12 weeks
Result:Reduced atherogenic lesion areas in the aortae and heart.
Animal Model:9-week old male ICR mice (pharmacokinetic analysis)[4]
Dosage:5 mg/kg ,10 mg/kg
Administration:Oral administration
Result:t1/2= 0.693/λ
分子量

583.63

性状

Solid

Formula

C31H37NO10

CAS 号

147444-03-9

结构分类
  • Terpenoids
  • Sesquiterpenes
来源

filamentous fungi

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month