2. Metabolic Enzyme/Protease GPCR/G Protein
  3. Phosphodiesterase (PDE) GPR35
  4. Zaprinast

Zaprinast  (Synonyms: M&B 22948)

Cat. No.: HY-B1816 Purity: 99.95%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Zaprinast Chemical Structure

Zaprinast Chemical Structure

CAS No. : 37762-06-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 50 In-stock
Solution
10 mM * 1 mL in DMSO USD 50 In-stock
Solid
5 mg USD 42 In-stock
10 mg USD 70 In-stock
50 mg USD 210 In-stock
100 mg USD 340 In-stock
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Based on 1 publication(s) in Google Scholar

Zaprinast Related Antibodies

Top Publications Citing Use of Products

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Description

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[1][2][3].

IC50 & Target[1][2]

PDE5

 

In Vitro

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.

Zaprinast Related Antibodies
In Vivo

Zaprinast (3 and 10 mg/kg; i.p.) enhances spatial memory in elevated plus maze (EPM) and diminishes exploratory activity in the Hughes box test[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male inbred BALB/c ByJ mice aged 7 weeks[5]
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.
Molecular Weight

271.27

Formula

C13H13N5O2
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C1C(N=NN2)=C2N=C(C3=CC=CC=C3OCCC)N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.95%

COA (254 KB) HNMR (275 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

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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Zaprinast Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zaprinast37762-06-4M&B 22948Phosphodiesterase (PDE)GPR35G Protein-Coupled Receptor 35cGMPPhosphodiesterasePDE5vessel remodelingantiproliferativeproapoptoticInhibitorinhibitorinhibit

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