Vericiguat is a potent and orally available stimulator of guanylate cyclase (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. Chronic oral treatment with Vericiguat (3 or 10 mg/kg, q.d.) results in a significant attenuation of blood pressure increase during the course of the study. Vericiguat (3 or 10 mg/kg) treatment leads to a significant reduction in kidney injury molecule Kim-1 and osteopontin expression which are used as biomarkers for renal injury and dysfunction.
| Molecular Weight | 426.38 |
| Formula | C19H16F2N8O2 |
| CAS Number | 1350653-20-1 |
| Solubility (25°C) | DMSO 65 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Guanylate Cyclase Products |
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| Cenderitide
Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). |
| Prepro-ANF (56-92), human
Prepro-ANF (56-92), human is a human atrial natriuretic factor precursor. |
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Guanylin (mouse, rat), a petide, is composed of 15 amino acids. |
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