Product Information Zaprinast CAS Registry No.: 37762-06-4 Formal Name: 3,6-dihydro-5-(2-propoxyphenyl)-7H- Synonyms: 2-(o-Propoxyphenyl)-8-azapurin-6-one, FW: 271.3 Purity: ≥98% Stability: Supplied as: Laboratory Procedures
For long term storage, we suggest that zaprinast be stored as supplied at -20°C. It should be stable for at least one
Zaprinast is supplied as a crystalline solid. A stock solution may be made by dissolving the zaprinast in an organic solvent
purged with an inert gas. Zaprinast is soluble in organic solvents such as DMSO and dimethyl formamide (DMF). The
solubility of zaprinast in these solvents is approximately 10 mg/ml.
Zaprinast is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, zaprinast should first
be dissolved in DMF and then diluted with the aqueous buffer of choice. Zaprinast has a solubility of approximately
0.5 mg/ml in a 1:1 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution
The cyclic nucleotide second messenger guanosine 3’5’-cyclic monophosphate (cGMP) is an important mediator of
signal transduction and hence a wide range of cellular processes. It can be generated by soluble guanylyl cyclase in response
to binding of nitric oxide and degraded via members of the phosphodiesterase (PDE) protein family. Zaprinast, the
compound from which sildenafil (Viagra™) was developed, is a cGMP-specific phosphodiesterase inhibitor. It moderately
inhibits PDE5 and PDE6 with IC50 values of 0.5-0.76 and 0.15 µM, respectively, and weakly inhibits PDE9, PDE10, and
PDE11 with IC50 values of 35, 22, and 11-33 µM, respectively.1,2 Zaprinast therefore enhances the vasodilatory effects
of nitric oxide in a range of vascular tissues by prolonging the cGMP-mediated activation of cGMP-dependent protein
kinase.2 Zaprinast also activates both the rat and human G protein-coupled receptor, GPR35 with EC50 values of 16 nM
References 1. Nakamizo, T., Kawamata, J., Yoshida, K., et al. Phosphodiesterase inhibitors are neuroprotective to cultured spinal
motor neurons. J. Neurosci. Res.71, 485-495 (2003).
2. Gibson, A. Phosphodiesterase 5 inhibitors and nitrergic transmission-from zaprinast to sildenafil. Eur. J. Pharmacol. 411, 1-10 (2001).
3. Taniguchi, Y., Tonai-Kachi, H., and Shinjo, K. Zaprinast, a well-known cyclic guanosine monophosphate-specific
phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett.580, 5003-5008 (2006). Cayman Chemical Related Products For a list of related pr Mailing address 1180 E. Ellsworth Road Ann Arbor, MI 48108 USA WARNING: ThIs pRoducT Is foR lAboRAToRy ReseARch oNly: NoT foR AdmINIsTRATIoN To humANs. NoT foR humAN oR veTeRINARy dIAGNosTIc oR TheRApeuTIc use. MATERIAL SAFETY DATA
This material should be considered hazardous until information to the contrary becomes available. Do not ingest, swallow, or inhale. Do not get in eyes, on skin, or on clothing. Wash thoroughly
after handling. This information contains some, but not all, of the information required for the safe and proper use of this material. Before use, the user must review the complete Material Safety Data
Sheet, which has been sent via email to your institution. WARRANTY AND LIMITATION OF REMEDY
Cayman Chemical Company makes no warranty or guarantee of any kind, whether written or oral, expressed or implied, including without limitation, any warranty of fitness for a particular
purpose, suitability and merchantability, which extends beyond the description of the chemicals hereof. Cayman warrants only to the original customer that the material will meet our specifications
Cayman will carry out its delivery obligations with due care and skill. Thus, in no event will Cayman have any obligation or liability, whether in tort (including negligence) or in contract, for
any direct, indirect, incidental or consequential damages, even if Cayman is informed about their possible existence.
This limitation of liability does not apply in the case of intentional acts or negligence of Cayman, its directors or its employees. exclusive remedy and Cayman’s sole liability hereunder shall be limited to a refund of the purchase price, or at Cayman’s option, the replacement, at no cost to Buyer, of all material that
Said refund or replacement is conditioned on Buyer giving written notice to Cayman within thirty (30) days after arrival of the material at its destination. Failure of Buyer to give said notice within
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