Home GPCR & G Protein Guanylate Cyclase agonist Vericiguat For research use only.

Vericiguat

Synonyms: BAY1021189

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

Vericiguat Chemical Structure

Vericiguat Chemical Structure

CAS: 1350653-20-1

Purity & Quality Control

Batch: Purity: 99.75%
99.75

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Biological Activity

Description Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase (sGC) stimulator.
Targets
sGC [1]
In vitro
In vitro

The stimulation of sGC by Vericiguat is examined with a recombinant CHO cell line overexpressing rat sGC. Vericiguat stimulates the sGC reporter cell line concentration dependently with an EC50 of 1005 ± 145 nM. In the presence of the NO donor S-nitroso-N-acetyl-D,L-penicillamine (SNAP) (30 and 100 nM), the EC50 value shifts to 39.0 ± 5.1 and 10.6 ± 1.7 nM, respectively. In the presence of ODQ, pretreatment of the sGC reporter cell line with 10 μM ODQ for 3 h results in a significantly reduced efficacy of Vericiguat, with an EC50 of 256 ± 40 nM being observed.[1]
Cell Research Cell lines CHO cells
Concentrations 0.01 μM to 100 μM
Incubation Time 6 min
Method

Cells are plated in a volume of 25 μL on white 384-well Greiner Bio-One microplates and are cultured for 1 or 2 d in medium. Medium is removed, and cells are loaded for 3 h with calcium-free Tyrode-containing coelenterazine. Serial dilutions of the test compounds (including Vericiguat) in a volume of 10 μL in calcium-free Tyrode are applied to the cells for 6 min. Thereafter, 35 μL of Tyrode-containing calcium (final concentration: 3 mM) is added to the cells and the emitted light is measured for 40 s using a CCD camera in a light-tight box. The minimal effective concentration (MEC) is determined as the concentration where a ≥3-fold increase in the basal luminescence value is observed.
In Vivo
In vivo

Vericiguat can maintain heart and kidney function in a model of hypertension-induced end-organ damage with substantially reduced overall mortality.[1]
Animal Research Animal Models renin transgenic rats (RenTG)
Dosages 3 mg/kg, 10 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06148935 Recruiting Chronic Heart Failure With Reduced Ejection Fraction Bayer November 30 2023 --
NCT05974189 Active not recruiting Chronic Heart Failure With Reduced Ejection Fraction Bayer July 11 2023 --
NCT05711719 Recruiting Metabolic Syndrome|Coronary Microvascular Dysfunction Johns Hopkins University|Merck Sharp & Dohme LLC June 16 2023 Phase 2
NCT05697640 Not yet recruiting Post-COVID ME/CFS Charite University Berlin Germany|Bayer February 2023 Phase 2
NCT05666518 Recruiting Chronic Heart Failure Bayer August 31 2022 --

Chemical lnformation & Solubility

Molecular Weight 426.38 Formula

C19H16F2N8O2
CAS No. 1350653-20-1 SDF --
Smiles COC(=O)NC1=C(N)N=C(N=C1N)C2=N[N](CC3=CC=CC=C3F)C4=NC=C(F)C=C24
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 85 mg/mL ( (199.35 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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