Zaprinast
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.
Product Specifications
CAS Number
37762-06-4
Product Name Alternative
M&B 22948
Purity
>98% (HPLC)
Solubility
In Vitro: DMSO : 62.5 mg/mL (230.40 mM)
Smiles
O=C1C (NN=N2) =C2NC (C3=CC=CC=C3OCCC) =N1
Molecular Formula
C13H13N5O2
Molecular Weight
271.3
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
3,6-dihydro-5- (2-propoxyphenyl) -7H-1,2,3-triazolo[4,5-d]pyrimidin-7-one
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