Vericiguat

Catalog No.S9693 Batch:S969301

Technical Data

Formula	C₁₉H₁₆F₂N₈O₂
Molecular Weight	426.38	CAS No.	1350653-20-1
Solubility (25°C)*	In vitro	DMSO	85 mg/mL (199.35 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]

In vivo

Vericiguat can maintain heart and kidney function in a model of hypertension-induced end-organ damage with substantially reduced overall mortality.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models renin transgenic rats (RenTG) Dosages 3 mg/kg, 10 mg/kg Administration Oral gavage

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
renin transgenic rats (RenTG)
Dosages
3 mg/kg, 10 mg/kg
Administration
Oral gavage

References

[1] Markus Follmann, et al. J Med Chem. 2017 Jun 22;60(12):5146-5161.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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