1. GPCR/G Protein
  2. Guanylate Cyclase
  3. Vericiguat

Vericiguat  (Synonyms: BAY1021189)

Cat. No.: HY-16774 Purity: 99.11%
COA Handling Instructions

Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.

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

Vericiguat Chemical Structure

Vericiguat Chemical Structure

CAS No. : 1350653-20-1

Size Price Stock Quantity
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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 143 In-stock
Solution
10 mM * 1 mL in DMSO USD 143 In-stock
Solid
2 mg USD 70 In-stock
5 mg USD 130 In-stock
10 mg USD 180 In-stock
50 mg USD 540 In-stock
100 mg USD 770 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Vericiguat:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.

In Vitro

Vericiguat (0.01 μM to 100 μM) stimulates recombinant sGC concentration dependently, by 1.7-fold to 57.6-fold. When combined with the NO donor diethylamine/nitric oxide complex (DEA/NO), vericiguat and DEA/NO have a synergistic effect on the enzyme activity over a wide range of concentrations. At highest concentrations of vericiguat (100 μM) and DEA/NO (100 nM), the specific activity of sGC is 341.6-fold above baseline. Vericiguat stimulates the sGC reporter cell line concentration dependently, with an EC50 of 1005±145 nM. Vericiguat inhibits phenylephrine-induced contractions of rabbit saphenous artery rings, rabbit aortic rings, and canine femoral vein rings concentration dependently, with IC50 values of 798, 692, and 3072 nM, respectively. Vericiguat inhibits the U46619-induced contractions of porcine coronary artery rings concentration dependently, with an IC50 of 956 nM[1].

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

In Vivo

Vericiguat (compound 24) (oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 days) maintains heart and kidney function in a model of hypertension-induced end-organ damage in L-NAME-treated renin transgenic rats. Additionally,Vericiguat-treated group substantially reduces overall mortality when compared to the control group[1].

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

Animal Model: L-NAME-treated renin transgenic rats[1]
Dosage: 3 mg/kg, 10 mg/kg
Administration: Oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 days
Result: Resulted in a significant attenuation of blood pressure increase, however the overall rise of blood pressure increase was not halted in the 3/10 mg/kg treatment groups.
Resulted a significant and dose-dependent reduction of heart hypertrophy, in both the right and left ventricle.
With respect to kidney damage, Vericiguat  Led to a significant reduction in kidney injury molecule Kim-1 and osteopontin expression which are used as biomarkers for renal injury and dysfunction.
Resulted in a significant and dose-dependent increase in survival rates. The rat survival rate was 70% and 90%, respectively in the 3 and 10 mg/kg qd treatment groups. In contrast, the survival rate in the placebo group was only 25% after 21 days.
Clinical Trial
Molecular Weight

426.38

Formula

C19H16F2N8O2

CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(OC)NC1=C(N)N=C(C2=NN(CC3=CC=CC=C3F)C4=NC=C(F)C=C42)N=C1N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 60 mg/mL (140.72 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 2.3453 mL 11.7266 mL 23.4533 mL
5 mM 0.4691 mL 2.3453 mL 4.6907 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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • 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: ≥ 2.5 mg/mL (5.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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).
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: 99.11%

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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3453 mL 11.7266 mL 23.4533 mL 58.6331 mL
5 mM 0.4691 mL 2.3453 mL 4.6907 mL 11.7266 mL
10 mM 0.2345 mL 1.1727 mL 2.3453 mL 5.8633 mL
15 mM 0.1564 mL 0.7818 mL 1.5636 mL 3.9089 mL
20 mM 0.1173 mL 0.5863 mL 1.1727 mL 2.9317 mL
25 mM 0.0938 mL 0.4691 mL 0.9381 mL 2.3453 mL
30 mM 0.0782 mL 0.3909 mL 0.7818 mL 1.9544 mL
40 mM 0.0586 mL 0.2932 mL 0.5863 mL 1.4658 mL
50 mM 0.0469 mL 0.2345 mL 0.4691 mL 1.1727 mL
60 mM 0.0391 mL 0.1954 mL 0.3909 mL 0.9772 mL
80 mM 0.0293 mL 0.1466 mL 0.2932 mL 0.7329 mL
100 mM 0.0235 mL 0.1173 mL 0.2345 mL 0.5863 mL
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Vericiguat 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.

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Vericiguat
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