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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-Zaprinast
Zaprinast

Chemical Structure : Zaprinast

CAS No.: 37762-06-4

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Zaprinast (M&B 22948)

货号: PC-70272Not For Human Use, Lab Use Only.

Zaprinast (M&B 22948) is a potent, cGMP-specific phosphodiesterase inhibitor with IC50 of 0.5-0.76 and 0.15 uM for PDE5 and PDE6 respectively, also is an agonist for GPR35 (EC50=16/840 nM for rat/human GPR35).

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50 mg ￥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Zaprinast (M&B 22948) is a potent, cGMP-specific phosphodiesterase inhibitor with IC50 of 0.5-0.76 and 0.15 uM for PDE5 and PDE6 respectively, also is an agonist for GPR35 (EC50=16/840 nM for rat/human GPR35).
Zaprinast weakly inhibits PDE9, PDE10, and PDE11 with IC50 of 10-30 uM.
Zaprinast enhances the vasodilatory effects of nitric oxide in a range of vascular tissues by prolonging the cGMP-mediated activation of cGMP-dependent protein kinase.
Zaprinast also reduces cellular 2HG levels by inhibiting the upstream enzyme glutaminase (GLS), reverses histone hypermethylation and soft-agar growth of IDH1-mutant cells.

物理化学性质&存储条件

分子量 271.3
分子式 C13H13N5O2
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

3,6-dihydro-5-(2-propoxyphenyl)-7H-1,2,3-triazolo[4,5-d]pyrimidin-7-one

参考文献

1. Elhammali A, et al. Cancer Discov. 2014 Jul;4(7):828-39.

2. Taniguchi Y, et al. FEBS Lett. 2006 Sep 18;580(21):5003-8.

3. Frossard N, et al. Br J Pharmacol. 1981 Aug;73(4):933-8.

4. Griffith TM, et al. Eur J Pharmacol. 1985 Jun 7;112(2):195-202.

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