Vericiguat

Research use only, not for human use.

Vericiguat (0.01 μM to 100 μM) stimulates recombinant sGC concentration dependently, by 1.7-fold to 57.6-fold.

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.(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.(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.

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.

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. Animal Model:L-NAME-treated renin transgenic ratsDosage:3 mg/kg, 10 mg/kg Administration: Oral administration; 3 mg/kg, 10 mg/kg; once daily; 21 daysResult: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.

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Metabolic Enzyme/Protease

Guanylate Cyclase

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1350653-20-1

426.38

C??H??F?N?O?

>98% (HPLC)

DMSO : 60 mg/mL (140.72 mM; Need ultrasonic)；H2O : < 0.1 mg/mL (insoluble)

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

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(-20℃)

With Ice Pack

≥ 2 years