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.
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- CAS. Nr.: 2170608-85-0
- Formel: C20H21N5O
- Molecular Weight:347.41
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Speicherung:
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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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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).
Chemical Information
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CAS. Nr. 2170608-85-0
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Molecular Weight 347.41
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PZ-3022 Related Classifications
HY-164909 Related Classifications
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