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

Vericiguat (Synonyms: BAY1021189)

Cat. No.: HY-16774 Purity: 99.09%
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

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10 mg USD 220 In-stock
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100 mg USD 950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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].

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.

1350653-20-1

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 60 mg/mL (140.72 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
10 mM 0.2345 mL 1.1727 mL 2.3453 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References

Purity: 99.09%

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Keywords:

VericiguatBAY1021189BAY 1021189BAY-1021189Guanylate CyclaseInhibitorinhibitorinhibit

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Product Name:
Vericiguat
Cat. No.:
HY-16774
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