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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 131863-75-7
- 分子式: C14H14ClN3
- 分子量:259.73
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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.
化学情報
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CAS 番号 131863-75-7
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分子量 259.73
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分子式 C14H14ClN3
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SMILES
N#CC1=CC=C(C=C1)[C@@H]2N3C(CCC2)=CN=C3.Cl
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別名
(R)-Fadrozole hydrochloride; (R)-CGS 16949A; FAD286 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Dexfadrostat hydrochloride 関連分類
HY-113986C 関連分類
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