Dexfadrostat hydrochloride  (Synonyms: (R)-Fadrozole hydrochloride; (R)-CGS 16949A; FAD286 hydrochloride)

Dexfadrostat ((R)-Fadrozole) hydrochloride is an orally active and selective aromatase inhibitor, with human aromatase IC₅₀ values of 6.4 nM. Dexfadrostat hydrochloride suppresses estrogen synthesis, reduces circulating estradiol levels and suppresses aldosterone production. Dexfadrostat hydrochloride can be used for the research of breast cancer, primary aldosteronism, and hypertension^[1][2][3][4].

Dexfadrostat (20 min) hydrochloride potently inhibits human placental aromatase in vitro with an IC₅₀ of 6.4 nM^[1].
Dexfadrostat hydrochloride potently inhibits rat ovarian aromatase in vitro^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dexfadrostat (Compound 26a) (p.o.; single dose) hydrochloride potently inhibits androstenedione-induced uterine hypertrophy in immature female rats with an oral ED₅₀ of 0.03 mg/kg^[1].
Dexfadrostat (p.o.) hydrochloride reduces circulating estradiol levels and suppresses uterine weight in intact cyclic female rats without inducing adrenal hypertrophy at doses that maximally inhibit estrogen synthesis^[1].
Dexfadrostat (p.o.; daily) hydrochloride exhibits potent antitumor efficacy in intact female rats with DMBA (HY-W011845)-induced mammary tumors^[1].
Dexfadrostat (0.01 μmol/kg; p.o.; single dose) hydrochloride significantly inhibits ovarian estrogen synthesis in female rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

259.73

C₁₄H₁₄ClN₃

131863-75-7

N#CC1=CC=C(C=C1)[C@@H]2N3C(CCC2)=CN=C3.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Browne LJ, et al. Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. J Med Chem. 1991;34(2):725-736.  [Content Brief]

  [2]. Mulatero P, et al. Safety and efficacy of once-daily dexfadrostat phosphate in patients with primary aldosteronism: a randomised, parallel group, multicentre, phase 2 trial. EClinicalMedicine. 2024;71:102576. Published 2024 Apr 6.

  [3]. Mulatero P, et al. CYP11B2 inhibitor dexfadrostat phosphate suppresses the aldosterone-to-renin ratio, an indicator of sodium retention, in healthy volunteers. Br J Clin Pharmacol. 2023;89(8):2483-2496.

  [4]. Pignatti E, et al. Structural and clinical characterization of CYP11B2 inhibition by dexfadrostat phosphate. J Steroid Biochem Mol Biol. 2023;235:106409.