131863-75-7
Chemical Structure
Dexfadrostat hydrochloride
Synonym(s): (R)-Fadrozole hydrochloride; (R)-CGS 16949A; FAD286 hydrochloride
- CAS No.: 131863-75-7
- Formula:C14H14ClN3
- Molecular Weight:259.73
InChIKey: UKCVAQGKEOJTSR-PFEQFJNWSA-N
SMILES: N#CC1=CC=C(C=C1)[C@@H]2N3C(CCC2)=CN=C3.Cl
Biological Activity: 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].
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Dexfadrostat 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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [4]. Pignatti E, et al. Structural and clinical characterization of CYP11B2 inhibition by dexfadrostat phosphate. J Steroid Biochem Mol Biol. 2023;235:106409. [Content Brief]
Keywords
