PZ-3022
PZ-3022 is an orally active allosteric agonist of pantothenate kinase (PanK) with an EC50 of 5.3 nM against PanK3. PZ-3022 antagonizes the inhibitory effect of C3-CoA. PZ-3022 increases CoA levels in cells and the liver, upregulates CoASH and C2-CoA, downregulates C3-CoA, and restores impaired TCA cycle and mitochondrial function. PZ-3022 can be used for the research of propionic acidemia and metabolic CoA deficiency.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- CAS 番号: 2170608-85-0
- 分子式: C20H21N5O
- 分子量:347.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
PZ-3022 potently activates purified human PanK3 with an EC50 of 5.3 nM via allosteric binding to the PanK dimer[1].
PZ-3022 effectively elevates total intracellular CoA in cultured human C3A hepatoma cells and protects all PanK isoforms from C3-CoA-mediated inhibition[1].
PZ-3022 (compound 1) potently inhibits purified PANK3 enzyme with a Ki value of 5.3 nM; it also inhibits purified PANK1β enzyme with a Ki value of 789 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pcca-/-PCCA(A138T)tg/0 (male and female, weaned at 21 days, analyzed at 70 days of age, propionic acidemia model)[1]
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Dosage:10 mg/kg (short-term); 30 mg/kg (short-term); 75 ppm (long-term)
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Administration:p.o.; 3 doses at 24-hour intervals (short-term); chow; daily; from weaning to 70 days of age (long-term)
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Result:Raises hepatic CoASH, C2-CoA and total CoA, lowers hepatic C3-CoA, and optimizes hepatic C3:C2-CoA ratio in PA mice (short-term 10 or 30 mg/kg).
Decreases plasma C3:C2-carnitine ratio in male PA mice (short-term 30 mg/kg).
Returns hepatic CoASH and C2-CoA to baseline levels, reduces hepatic C3-CoA and hepatic C3:C2-CoA ratio in PA mice (long-term 75 ppm).
Modulates liver and plasma carnitine levels and cuts plasma C3:C2-carnitine ratio in PA mice of both sexes (long-term 75 ppm).
Lowers urinary TCA cycle metabolites with an 80% drop in malate and normalizes heart:body weight ratio in PA mice (long-term 75 ppm).
化学情報
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CAS 番号 2170608-85-0
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分子量 347.41
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分子式 C20H21N5O
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SMILES
N#CC1=NN=C(N2CCN(CC2)C(CC3=CC=C(C4CC4)C=C3)=O)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PZ-3022 関連分類
HY-164909 関連分類
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