Zaprinast

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Zaprinast (M&B 22948) 是一种有效的 cGMP 特异性磷酸二酯酶抑制剂，对 PDE5 和 PDE6 的 IC50 分别为 0.5-0.76 和 0.15 uM。

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); weakly inhibits PDE9, PDE10, and PDE11 with IC50 of 10-30 uM; enhances the vasodilatory effects of nitric oxide in a range of vascular tissues by prolonging the cGMP-mediated activation of cGMP-dependent protein kinase; also reduces cellular 2HG levels by inhibiting the upstream enzyme glutaminase (GLS), reverses histone hypermethylation and soft-agar growth of IDH1-mutant cells.Asthma Discontinued.

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Animal Model:Male inbred BALB/c ByJ mice aged 7 weeks Dosage:3 and 10 mg/kg Administration:IP; 60 min before the first session Result: Significantly decreased second-day latency compared to the control group in the EPM test with 10 mg/kg. Significantly shortened the time spent in the novel side in the Hughes box with 10 mg/kg.

M&B 22948

Angiogenesis

PDE

PDE

Inflammation/Immunology

Asthma

37762-06-4

271.3

C13H13N5O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (230.40 mM)

O=C1C(NN=N2)=C2NC(C3=CC=CC=C3OCCC)=N1

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

(-20℃)

With Ice Pack

≥ 2 years