啶南平 A

生物活性靶点体外研究体内研究啶南平 A 试剂级价格

啶南平 A

CAS号:147444-03-9
英文名:pyripyropene A
中文名:啶南平 A
CBNumber:CB91387745
分子式:C31H37NO10
分子量:583.63
MOL File:147444-03-9.mol

啶南平 A化学性质

熔点 :153-154℃
沸点 :690.8±55.0 °C(Predicted)
密度 :1.33±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C, protect from light, stored under nitrogen
溶解度 :DMSO: Soluble; Methanol: Soluble
酸度系数(pKa) :11.72±0.70(Predicted)
形态 :White to brown powder.
颜色 :Pale pink to rusty brown

啶南平 A性质、用途与生产工艺

生物活性 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。
靶点

IC50: 0.07 µM (ACAT2)

体外研究

Pyripyropene A (0-100 µM; 72 hours) exhibits anti-proliferative activity against HUVECs, and with an IC ₅₀ value of 1.8 µM.
Pyripyropene A (10 µM ; 24 hours) inhibits VEGF (20 ng/ml)-induced migration and tubular formation of HUVECs in dose-dependent fashion.
Pyripyropene A do not show growth inhibitory effects against KB3-1, K562 and Neuro2A cells.

Cell Proliferation Assay

Cell Line:	HUVECs
Concentration:	0-100 µM
Incubation Time:	72 hours
Result:	Exhibited anti-proliferative activity against HUVECs with an IC ₅₀ value of 1.8 µM.

体内研究

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.
Pyripyropene A inhibits the hepatic e acyl–coenzyme A:cholesterol acyltransferase 2 (ACAT2) activity in vivo.
Pyripyropene A displays a half-life (t _1/2 ) of 0.693/λ, where λ represented the terminal slope of the log-linear portion of concentration time profile.

Animal Model:	Male C57BL/6 mice
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.