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Biological Activity: Zaprinast inhibits PDE5 and PDE6 with IC50 values of 0.5-0.76 µM and0.15 µM, respectively.
CAS Number: 37762-06-4
Description: Zaprinast is a cGMP-specific PDE inhibitor which moderately inhibits PDE5 and PDE6. It weakly inhibits PDE9, PDE10 and PDE11. Sildenafil (Viagra™) was developed from Zaprinast, which 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, GPR35 is activated by Zaprinast.
Format: A crystalline solid
Purity: ≥98% by HPLC
Solubility: Soluble in DMSO and DMF, purged with an inert gas. Solubility in DMSO and DMFis ~10 mg/ml. For maximum solubility, dissolve in DMF and then dilute with the aqueous bufferof choice.
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Biosafety Level: Not applicable (BSL-1)
References: 1. Nakamizo, T., et al., J. Neurosci. Res. 2003;71:485-495.
2. Gibson, A., et al., Eur. J. Pharmacol. 2001;411:1-10.
3. Taniguchi, Y., et al., FEBS Lett. 2006;580:5003-5008.
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