Pyripyropene A
Based on 1 publication(s) in Google Scholar
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.37%
- CAS 番号: 147444-03-9
- 分子式: C31H37NO10
- 分子量:583.63
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Pyripyropene A
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生物活性
製品説明
IC50 & Target
IC50: 0.07 µM (ACAT2)[1]
体外実験
Pyripyropene A (0-100 μM; 72 hours) exhibits anti-proliferative activity against HUVECs, and with an IC50 value of 1.8 μM[1].
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Pyripyropene A (10 μM ; 24 hours) inhibits VEGF (20 ng/ml)-induced migration and tubular formation of HUVECs in dose-dependent fashion[1].
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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. Further protocols information, click here.
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Cell Line:HUVECs
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Concentration:0-100 µM
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Incubation Time:72 hours
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Result:Exhibited anti-proliferative activity against HUVECs with an IC50 value of 1.8 µM.
体内実験
? 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.
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Animal Model:Male C57BL/6 mice[2]
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Dosage:0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg
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Administration:Oral administration; daily; for 12 weeks
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Result:Reduced atherogenic lesion areas in the aortae and heart.
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Animal Model:9-week old male ICR mice (pharmacokinetic analysis)[4]
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Dosage:5 mg/kg ,10 mg/kg
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Administration:Oral administration
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Result:t1/2 = 0.693/λ
化学情報
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CAS 番号 147444-03-9
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性状 Solid
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分子量 583.63
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分子式 C31H37NO10
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Color White to light yellow
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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
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Structure Classification
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Initial Source
filamentous fungi
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
Transcription factor ETV4 plays a critical role in the development of non-alcoholic fatty liver disease. [Abstract]2024 Dec;282(Pt 5):137235. PMID: 39500423
溶剤 & 溶解度
体外:
Methanol : 10 mg/mL (17.13 mM; Need ultrasonic and warming)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hayashi A, et al. Pyripyropenes, fungal sesquiterpenes conjugated with alpha-pyrone and pyridine moieties, exhibits anti-angiogenic activity against human umbilical vein endothelial cells. Biol Pharm Bull. 2009 Jul;32(7):1261-5. [Content Brief]
[2]. Ohtawa M, et al. Design and Synthesis of A-Ring Simplified Pyripyropene A Analogues as Potent and Selective Synthetic SOAT2 Inhibitors. ChemMedChem. 2018 Mar 6;13(5):411-421. [Content Brief]
[3]. Ohshiro T, et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15. [Content Brief]
[4]. Lee KR , et al. Determination of Penicillium griseofulvum-oriented pyripyropene A, a selective inhibitor of acyl-coenzyme A:cholesterol acyltransferase 2, in mouse plasma using liquid chromatography-tandem mass spectrometry and its application to pharmacokinetic studies. Biomed Chromatogr. 2019 Feb;33(2):e4388. [Content Brief]
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 |
Pyripyropene A 関連分類
HY-117832 関連分類
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