Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Zaprinast is a potent phosphodiesterase (PDE) inhibitor with selectivity for PDE5, PDE6, PDE9 and PDE11 and IC₅₀ values of 0.76, 0.15, 29.0, and 12.0 μM, respectively. It was an unsuccessful clinical drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil, which successfully reached the market. As an inhibitor of the growth of asexual blood-stage malaria parasites (P. falciparum), it inhibits PfPDE1 and activates GPR35.
ln Vitro |
In transfectants coexpressing FLAG-hGPR35 and four exogenous Gα proteins, zaprinast (0.1, 0.3, 1, 3, 10, 30 μM) induces intracellular excitation in a concentration-dependent manner in HEK293 cells [2]. Zaprinast (100 μM; 5 minutes) can promote the phosphorylation of five different cells in the C-terminal tail of human GPR35a in HEK293T cells [4].
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ln Vivo |
Zaprinast (3 and 10 mg/kg; i.p.) decreases exploratory activity in the Hughes box test and increases spatial memory in the elevated plus maze (EPM) [5].
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Animal Protocol |
Animal/Disease Models: 7-year-old male inbred BALB/c ByJ mice [5]
Doses: 3 and 10 mg/kg Route of Administration: IP; 60 minutes before first treatment Experimental Results: In the EPM test at 10 mg/kg , the incubation period on the second day was Dramatically shortened compared with the control group. 10 mg/kg Dramatically shortened the time spent in the Hughes box on the new side. |
References |
[1]. Choi SH , et al. Zaprinast, an inhibitor of cGMP-selective phosphodiesterases, enhances the secretion of TNF-alpha and IL-1beta and the expression of iNOS and MHC class II molecules in rat microglial cells. J Neurosci Res. 2002 Feb 1;67(3):411-21.
[2]. Taniguchi Y, et al. Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett. 2006 Sep 18;580(21):5003-8. Epub 2006 Aug 17. [3]. Keswani AN , et al The cyclic GMP modulators YC-1 and zaprinast reduce vessel remodeling through antiproliferative and proapoptotic effects. J Cardiovasc Pharmacol Ther. 2009 Jun;14(2):116-24. [4]. Nina Divorty, et al. Agonist-induced phosphorylation of orthologues of the orphan receptor GPR35 functions as an activation sensor. J Biol Chem. 2022 Mar;298(3):101655. [5]. Furuzan Akar, et al. Zaprinast and rolipram enhances spatial and emotional memory in the elevated plus maze and passive avoidance tests and diminishes exploratory activity in naive mice. Med Sci Monit Basic Res. 2014 Jul 24:20:105-11. |
Molecular Formula |
C13H13N5O2
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Molecular Weight |
271.27462
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CAS # |
37762-06-4
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CCCOC1=CC=CC=C1C1=NC(=O)C2=NNNC2=N1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~230.40 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6864 mL | 18.4318 mL | 36.8636 mL | |
5 mM | 0.7373 mL | 3.6864 mL | 7.3727 mL | |
10 mM | 0.3686 mL | 1.8432 mL | 3.6864 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.