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

Pyripyropene A is an orally active, 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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250 μg USD 490 In-stock

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Based on 1 publication(s) in Google Scholar

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Description

Pyripyropene A is an orally active, 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to light yellow

SMILES

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

Structure Classification
Initial Source

filamentous fungi

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

Methanol : 10 mg/mL (17.13 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7134 mL 8.5671 mL 17.1341 mL
5 mM 0.3427 mL 1.7134 mL 3.4268 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.71%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Methanol 1 mM 1.7134 mL 8.5671 mL 17.1341 mL 42.8354 mL
5 mM 0.3427 mL 1.7134 mL 3.4268 mL 8.5671 mL
10 mM 0.1713 mL 0.8567 mL 1.7134 mL 4.2835 mL
15 mM 0.1142 mL 0.5711 mL 1.1423 mL 2.8557 mL
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Pyripyropene A Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Pyripyropene A
Cat. No.:
HY-117832
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