1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. Pyripyropene A

Pyripyropene A 

Cat. No.: HY-117832 Purity: >97.0%
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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.

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Pyripyropene A Chemical Structure

Pyripyropene A Chemical Structure

CAS No. : 147444-03-9

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Description

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[1][2][3][4].

IC50 & Target

IC50: 0.07 µM (ACAT2)[1]

In Vitro

Pyripyropene A (0-100 µM; 72 hours) exhibits anti-proliferative activity against HUVECs, and with an IC50 value 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 IC50 value of 1.8 µM.
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
Molecular Weight

583.63

Formula

C₃₁H₃₇NO₁₀

CAS No.

147444-03-9

SMILES

O=C1OC(C2=CC=CN=C2)=CC3=C1[[email protected]](O)[[email protected]@]4([H])[[email protected]]([[email protected]@H](OC(C)=O)C[[email protected]@]5([H])[[email protected]](C)(COC(C)=O)[[email protected]@H](OC(C)=O)CC[[email protected]@]54C)(C)O3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

References

Purity: >97.0%

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Keywords:

Pyripyropene AAcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseSOAT2ACAT2hypercholesterolemiaatherosclerosisInhibitorinhibitorinhibit

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Pyripyropene A
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