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PZ-3022

Chemical Structure : PZ-3022

CAS No.: 2170608-85-0

PZ-3022 (PZ3022)

Catalog No.: PC-28328Not For Human Use, Lab Use Only.

PZ-3022 is an allosteric, orally bioavailable Pantothenate kinase (PanK) activator with EC50 of 5.3 nM against PanK3, shows a lower affinity for PanK isoforms PANK1β and PANK2m with EC50 of 789 nM and 15 nM respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PZ-3022 is an allosteric, orally bioavailable Pantothenate kinase (PanK) activator with EC50 of 5.3 nM against PanK3, shows a lower affinity for PanK isoforms PANK1β and PANK2m with EC50 of 789 nM and 15 nM respectively.
PZ-3022 renders PanK resistant to C3-CoA inhibition in vitro.
PZ-3022 (10 or 30 mg/kg) relieves CoASH sequestration in liver by increasing hepatic CoASH and C2-CoA and decreasing C3-CoA, consistent with the stimulation of TCA cycle flux.
PZ-3022 relieved hepatic CoA sequestration and elevated CoASH and C2-CoA in male propionic acidemia (PA) mice.
PZ-3022 allosterically activates PanK to counteract its inhibition by C3-CoA and normalizes the intracellular concentrations of total CoA, CoASH, and C2-CoA, and reduces C3-CoA in PA liver.

Physicochemical Properties

M.Wt 347.42
Formula C20H21N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

6-[4-[2-(4-Cyclopropylphenyl)acetyl]-1-piperazinyl]-3-pyridazinecarbonitrile

References

1. Subramanian C, et al. Sci Transl Med. 2021 Sep 15;13(611):eabf5965.

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