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.
For research use only. We do not sell to patients.
- CAS No.: 131863-75-7
- Formula: C14H14ClN3
- Molecular Weight:259.73
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Aromatase 6.4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| JEG-3 | IC50 |
680 nM
Compound: (R)-fadrazole HCl
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Inhibition of aromatase activity in human JEG3 cells
Inhibition of aromatase activity in human JEG3 cells
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[PMID: 18590272] |
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 (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.
Chemical Information
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CAS No. 131863-75-7
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Molecular Weight 259.73
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Formula C14H14ClN3
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SMILES
N#CC1=CC=C(C=C1)[C@@H]2N3C(CCC2)=CN=C3.Cl
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Synonyms
(R)-Fadrozole hydrochloride; (R)-CGS 16949A; FAD286 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dexfadrostat hydrochloride Related Classifications
HY-113986C Related Classifications
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