|6-(4-(2-(4-异丙基苯基)乙酰基)哌嗪-1-基)哒嗪-3-甲腈|CsnPharm

CAS No.: 2170608-82-7

PZ-2891 Catalog No. CSN23789

Synonyms: PZ-2891

PZ-2891 is a specific and brain-permeable Pantothenate kinase (PANK) modulator, acting as an orthosteric inhibitor with IC50 of 1.3 nM for hPANK3 and also an allosteric activator of PANK3 activity in the presence of acetyl-CoA in biochemical assays.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述PANK (Pantothenate kinase) is a metabolic enzyme that regulates cellular coenzyme A (CoA) levels, inactivating of which could lead to pantothenate kinase associated neurodegeneration. PZ-2891 is a brain-permeable allosteric PANK activator with IC50 value of 1.3nM for PANK3. PZ-2891 stabilized PANK3 by ∼7 °C in a cellular thermal shift (CETSA) assay and increased total intracellular CoA levels at concentration of 10μM in a human liver-derived cell line post 24h. Oral administration of PZ-2891 at dose of 15mg/kg and 20mg/kg every 12 h for 5 doses activated CoA synthesis in liver, forebrain and hindbrain of mice dosed with 100mg/kg pantothenate. Therapy with PZ-2891 rescued the weight loss, severe locomotor impairment and early death of a knockout mouse model of brain CoA deficiency.
作用机制PZ-2891 occupies the pantothenate pocket and engages the dimer interface to form a PANK•ATP•Mg2+•PZ-2891 complex. The binding of PZ-2891 to one protomer locks the opposite protomer in a catalytically active conformation that is refractory to acetyl-CoA inhibition.^[1]
动物研究
剂量
Mice: 30 mg/kg^[1] (p.o.)
参考文献

动物研究
剂量	Mice: 30 mg/kg^[1] (p.o.)

[1] Sharma LK, Subramanian C, et al. A therapeutic approach to pantothenate kinase associated neurodegeneration. Nat Commun. 2018 Oct 23;9(1):4399.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8618 mL
- 14.3090 mL
- 28.6181 mL
- 5 mM
- 0.5724 mL
- 2.8618 mL
- 5.7236 mL
- 10 mM
- 0.2862 mL
- 1.4309 mL
- 2.8618 mL

技术信息

CAS号

2170608-82-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H23N5O

运输

蓝冰

分子量

349.43

别名

PZ-2891

溶解度

DMSO	73.0 mg/mL (208.9 mM) warming
Water	Insoluble

动物实验配方

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