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PZ-2891

Chemical Structure : PZ-2891

CAS No.: 2170608-82-7

PZ-2891 (PZ2891)

货号: PC-35831Not For Human Use, Lab Use Only.

PZ-2891 (PZ2891) a specific, allosteric, BBB-permeable, orally active Pantothenate kinase (PANK) modulator, acting as both an orthosteric inhibitor (IC50=1.3 nM, hPANK3) and an allosteric activator of PANK3 activity in the presence of acetyl-CoA in biochemical assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PZ-2891 (PZ2891) a specific, allosteric, BBB-permeable, orally active Pantothenate kinase (PANK) modulator, acting as both an orthosteric inhibitor (IC50=1.3 nM, hPANK3) and an allosteric activator of PANK3 activity in the presence of acetyl-CoA in biochemical assays.
PZ-2891 occupies the pantothenate pocket and engages the dimer interface to form a PANK•ATP•Mg2+•PZ-2891 complex.
PZ-2891 inhibits all 3 human and mouse pantothenate kinase isoforms (hPANK1α IC50=40.2 nM, hPANK2 IC50=0.7 nM).
PZ-2891 increases intracellular CoA in cultured cells and elevates CoA levels in mouse liver and brain, improves gain weight, locomotor activity and life span in mouse model of brain CoA deficiency.

物理化学性质&存储条件

分子量 349.438
分子式 C20H23N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(4-(2-(4-isopropylphenyl)acetyl)piperazin-1-yl)pyridazine-3-carbonitrile

参考文献

1. Sharma LK, et al. Nat Commun. 2018 Oct 23;9(1):4399.

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