Zaprinast

SKU: orb1225158

Description

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.

Key Properties

• CAS Number: 37762-06-4
• MW: 271.3
• Purity: >98% (HPLC)
• Formula: C₁₃H₁₃N₅O₂
• SMILES: O=C1C(NN=N2)=C2NC(C3=CC=CC=C3OCCC)=N1
• Target: PDE
• Solubility: In Vitro: DMSO : 62.5 mg/mL (230.40 mM)

Bioactivity

• In Vivo:
  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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

M&B 22948

Quick Database Links

Gene Symbol

PDE