Pyripyropene A 是一种有效的选择性甾醇 O-酰基转移酶 2 (SOAT2)/酰基辅酶 A:胆固醇酰基转移酶 2 (ACAT2) 抑制剂，IC50 为 0.07 μM。
| Cas No. | 147444-03-9 |
| 别名 | 啶南平A |
| 化学名 | 3,6-bis(acetyloxy)-4-[(acetyloxy)methyl]-1,3S,4R,4aR,5,6S,6aS,12R,12aS,12bS-decahydro-12-hydroxy-4,6a,12b-trimethyl-9-(3-pyridinyl)-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-11-one |
| Canonical SMILES | O=C1OC(C2=CN=CC=C2)=CC3=C1[C@H](O)[C@@]4([H])[C@@](O3)(C)[C@@H](OC(C)=O)C[C@@]5([H])[C@@](COC(C)=O)(C)[C@@H](OC(C)=O)CC[C@@]54C |
| 分子式 | C31H37NO10 |
| 分子量 | 583.6 |
| 溶解度 | DMSO: Soluble,Methanol: Soluble |
| 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Acyl-CoA: cholesterol acyltransferase (ACAT) is a key enzyme for cholesteryl ester accumulation in atherogenesis, lipoprotein formation in liver, and cholesterol absorption from intestines, all of which are events that contribute to the atherosclerotic process. Two ACAT isozymes have been identified and are expressed in distinct tissues. ACAT1 is ubiquitously expressed at a high level in sebaceous glands, steroidogenic tissues, and macrophages, whereas ACAT2 is expressed predominantly in the liver and intestine. Pyripyropene A, naturally produced by A. fumigates, is a potent inhibitor of ACAT2 with an IC50 value of 70 nM in an in vitro activity assay. It demonstrates high selectivity for the ACAT2 isozyme, inhibiting ACAT1 in a similar assay with an IC50 value of >80 μM.A dose of 10 to 100 mg/kg PPPA inhibits cholesterol absorption in mouse intestine by 30.5-55%. Oral administration to apolipoprotein E-knockout mice at 10-50 mg/kg per day for 12 weeks can lower the levels of plasma cholesterol and hepatic cholesterol, very-low-density lipoprotein, and LDL content, resulting in protection from atherosclerosis development. |
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