Zaprinast
Based on 3 publication(s) in Google Scholar
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
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- Purity: 99.83%
- CAS No.: 37762-06-4
- 화학식: C13H13N5O2
- 분자량:271.27
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보관:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Zaprinast
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Biological Activity
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PDE5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.0611 μM
Compound: 3
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Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
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[PMID: 23713606] |
| CHO | EC50 |
0.98 μM
Compound: 3
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Agonist activity at mouse GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at mouse GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
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[PMID: 23713606] |
| CHO | EC50 |
1.96 μM
Compound: 3
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Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
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[PMID: 23713606] |
| CHO | EC50 |
2.24 μM
Compound: 3
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Agonist activity at human GPR35b expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at human GPR35b expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
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[PMID: 23713606] |
| HepG2 | IC50 |
>10 μM
Compound: 92125335
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HARVARD: Cytotoxicity in HepG2 cell line
HARVARD: Cytotoxicity in HepG2 cell line
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[PMID: 22586124] |
| HepG2 | IC50 |
7.79 μM
Compound: 92125335
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HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
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[PMID: 22586124] |
| HT-29 | EC50 |
0.11 μM
Compound: Zaprinast
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Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis
Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis
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10.1039/C2MD20210G |
| HT-29 | EC50 |
0.14 μM
Compound: Zaprinast
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Agonist activity at GPR35 in human HT-29 cells measured after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells measured after 10 mins by dynamic mass redistribution assay
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[PMID: 24900508] |
| HT-29 | EC50 |
0.16 μM
Compound: zaprinast
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Agonist activity at GPR35 in human HT-29 cells after 1 hr by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells after 1 hr by dynamic mass redistribution assay
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[PMID: 21950657] |
| HT-29 | EC50 |
0.16 μM
Compound: Zaprinast
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Agonist activity at GPR35 in human HT-29 cells by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells by dynamic mass redistribution assay
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[PMID: 22572579] |
| HT-29 | EC50 |
0.16 μM
Compound: Zaprinast
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Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
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[PMID: 24900447] |
| HT-29 | IC50 |
1.22 μM
Compound: zaprinast
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Agonist activity at GPR35 in human HT-29 cells assessed as desensitization of 1 uM zaprinast-induced DMR after 1 hr by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells assessed as desensitization of 1 uM zaprinast-induced DMR after 1 hr by dynamic mass redistribution assay
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[PMID: 21950657] |
| HT-29 | IC50 |
1.22 μM
Compound: Zaprinast
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Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
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[PMID: 24900447] |
| HT-29 | IC50 |
10.5 μM
Compound: zaprinast
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Antagonist activity at GPR35 in human HT-29 cells assessed as inhibition of zaprinast-induced DMR by dynamic mass redistribution assay
Antagonist activity at GPR35 in human HT-29 cells assessed as inhibition of zaprinast-induced DMR by dynamic mass redistribution assay
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[PMID: 21950657] |
| U2OS | EC50 |
3.25 μM
Compound: Zaprinast
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Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay
Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay
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10.1039/C2MD20210G |
| U2OS | EC50 |
4.2 μM
Compound: zaprinast
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Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and GPR35-GA14-VP16 transcription factor fusion protein assessed as transcriptional activation after 5 hrs by tango beta-arrestin translocation reporter assay
Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and GPR35-GA14-VP16 transcription factor fusion protein assessed as transcriptional activation after 5 hrs by tango beta-arrestin translocation reporter assay
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[PMID: 21950657] |
| U2OS | EC50 |
5.3 μM
Compound: Zaprinast
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Agonist activity at human GPR35 expressed in U2OS cells coexpressing Gal4-VP16/beta-arrestin fusion protein after 5 hrs by tango beta-arrestin translocation reporter gene assay
Agonist activity at human GPR35 expressed in U2OS cells coexpressing Gal4-VP16/beta-arrestin fusion protein after 5 hrs by tango beta-arrestin translocation reporter gene assay
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[PMID: 24900508] |
| U2OS | EC50 |
6.1 μM
Compound: Zaprinast
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Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
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[PMID: 24900447] |
| U2OS | EC50 |
6.2 μM
Compound: Zaprinast
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Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and Gal4-VP16 transcription factor assessed as beta arrestin translocation after 5 hrs by Tango assay
Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and Gal4-VP16 transcription factor assessed as beta arrestin translocation after 5 hrs by Tango assay
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[PMID: 22572579] |
Zaprinast (0.1, 0.3, 1, 3, 10, 30 μM) induces intracellular calcium mobilization in the transfectant coexpressing FLAG-hGPR35 and the four exogenous Gα proteins in a concentration-dependent manner in HEK293 cells[2].
Zaprinast (100 μM; 5 min) can promote phosphorylation of five distinct amino acids in the C-terminal tail of human GPR35a in HEK293T cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male inbred BALB/c ByJ mice aged 7 weeks[5]
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Dosage:3 and 10 mg/kg
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Administration:IP; 60 min before the first session
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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.
Chemical Information
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CAS No. 37762-06-4
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Appearance Solid
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분자량 271.27
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화학식 C13H13N5O2
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Color Off-white to pink
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SMILES
O=C1C(N=NN2)=C2N=C(C3=CC=CC=C3OCCC)N1
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Synonyms
M&B 22948
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Inhibiting HMGB1/AGER/NF-κB pathway prevents pro-inflammatory microglia polarization and protect photoreceptors in retinitis pigmentosa. [Abstract]2025 Feb 3:149:114192. PMID: 39904032 -
Mol Neurobiol
Hippocampal GPR35 Participates in the Pathogenesis of Cognitive Deficits and Emotional Alterations Induced by Aβ1-42 in Mice. [Abstract]2025 Jan;62(1):557-582. PMID: 38878116 -
용액&용해도
DMSO : 62.5 mg/mL (230.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6864 mL | 18.4318 mL | 36.8636 mL | 92.1591 mL |
| 5 mM | 0.7373 mL | 3.6864 mL | 7.3727 mL | 18.4318 mL | |
| 10 mM | 0.3686 mL | 1.8432 mL | 3.6864 mL | 9.2159 mL | |
| 15 mM | 0.2458 mL | 1.2288 mL | 2.4576 mL | 6.1439 mL | |
| 20 mM | 0.1843 mL | 0.9216 mL | 1.8432 mL | 4.6080 mL | |
| 25 mM | 0.1475 mL | 0.7373 mL | 1.4745 mL | 3.6864 mL | |
| 30 mM | 0.1229 mL | 0.6144 mL | 1.2288 mL | 3.0720 mL | |
| 40 mM | 0.0922 mL | 0.4608 mL | 0.9216 mL | 2.3040 mL | |
| 50 mM | 0.0737 mL | 0.3686 mL | 0.7373 mL | 1.8432 mL | |
| 60 mM | 0.0614 mL | 0.3072 mL | 0.6144 mL | 1.5360 mL | |
| 80 mM | 0.0461 mL | 0.2304 mL | 0.4608 mL | 1.1520 mL | |
| 100 mM | 0.0369 mL | 0.1843 mL | 0.3686 mL | 0.9216 mL |
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