Pyripyropene A

Pyripyropene A is a potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC50 of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo.

Product information

CAS Number: 147444-03-9

Molecular Weight: 583.63

Formula: C31H37NO10

Chemical Name: [(5aS,6S,7aR,8R,9S,11aS,11bS,12R)-6,9-bis(acetyloxy)-12-hydroxy-5a,8,11a-trimethyl-1-oxo-3-(pyridin-3-yl)-1,5a,6,7,7a,8,9,10,11,11a,11b,12-dodecahydro-2,5-dioxatetraphen-8-yl]methyl acetate

Smiles: C[C@]12CC[C@H](OC(C)=O)[C@@](C)(COC(C)=O)[C@@H]1C[C@H](OC(C)=O)[C@@]1(C)OC3C=C(OC(=O)C=3[C@H](O)[C@H]21)C1=CN=CC=C1

InChiKey: PMMQOFWSZRQWEV-RVTXXDJVSA-N

InChi: InChI=1S/C31H37NO10/c1-16(33)38-15-30(5)22-13-24(40-18(3)35)31(6)27(29(22,4)10-9-23(30)39-17(2)34)26(36)25-21(42-31)12-20(41-28(25)37)19-8-7-11-32-14-19/h7-8,11-12,14,22-24,26-27,36H,9-10,13,15H2,1-6H3/t22-,23+,24+,26+,27-,29+,30+,31-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Pyripyropene A (0-100 µM; 72 hours) exhibits anti-proliferative activity against HUVECs, and with an IC50 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.

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. Pyripyropene A inhibits the hepatic e acyl–coenzyme A:cholesterol acyltransferase 2 (ACAT2) activity in vivo. 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.

Products are for research use only. Not for human use.