啶南平 A
中文名称 | 啶南平 A |
---|---|
中文同义词 | 啶南平 A;化合物 T12592 |
英文名称 | pyripyropene A |
英文同义词 | pyripyropene A;FO 1289A;2H,11H-Naphtho[2,1-b]pyrano[3,4-e]pyran-11-one, 3,6-bis(acetyloxy)-4-[(acetyloxy)methyl]-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-12-hydroxy-4,6a,12b-trimethyl-9-(3-pyridinyl)-, (3S,4R,4aR,6S,6aS,12R,12aS,12bS)- |
CAS号 | 147444-03-9 |
分子式 | C31H37NO10 |
分子量 | 583.63 |
EINECS号 | |
相关类别 | |
Mol文件 | 147444-03-9.mol |
结构式 |
啶南平 A 性质
熔点 | 153-154℃ |
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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:可溶;甲醇:可溶 |
酸度系数(pKa) | 11.72±0.70(Predicted) |
形态 | 白色至棕色粉末。 |
颜色 | 淡粉色至铁锈棕色 |
IC50: 0.07 µM (ACAT2)
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. |
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. |
Animal Model: | 9-week old male ICR mice (pharmacokinetic analysis) |
Dosage: | 5 mg/kg ,10 mg/kg |
Administration: | Oral administration |
Result: | t 1/2 = 0.693/λ |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/01/25 | HY-117832 | 啶南平 A Pyripyropene A | 147444-03-9 | 250 μg | 4900元 |