Dexfadrostat (FAD-286) is a highly selective and potent non-steroidal inhibitor of aldosterone synthase (CYP11B2), with significant suppression of aldosterone production demonstrated in both in vitro and in vivo studies. It exhibits an IC₅₀ of approximately 4.2 nM for human CYP11B2, showing over 100-fold selectivity over 11β-hydroxylase (CYP11B1), which is critical for avoiding cortisol suppression. In rodent and primate models, FAD-286 effectively reduced plasma aldosterone levels without markedly affecting cortisol or corticosterone, confirming its potential utility in treating conditions such as primary aldosteronism, hypertension, and heart failure driven by aldosterone excess.
MedKoo Cat#: 125313
Name: Dexfadrostat HCl
CAS#: 131863-75-7 (HCl)
Chemical Formula: C14H14ClN3
Exact Mass: 259.0900
Molecular Weight: 259.74
Elemental Analysis: C, 64.74; H, 5.43; Cl, 13.65; N, 16.18
The following data is based on the product molecular weight 259.74 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
