Dexfadrostat
Based on 1 Customer Validation
Dexfadrostat ((R)-Fadrozole) is an orally active and selective aromatase inhibitor, with human aromatase IC50 values of 6.4 nM. Dexfadrostat suppresses estrogen synthesis, reduces circulating estradiol levels and suppresses aldosterone production. Dexfadrostat can be used for the research of breast cancer, primary aldosteronism, and hypertension.
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- Purity: 98.75%
- CAS No.: 102676-87-9
- 화학식: C14H13N3
- 분자량:223.27
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Aromatase 6.4 nM (IC50) |
Dexfadrostat (p.o.) 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) 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) 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.
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Animal Model:SHHF rats[2]
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Dosage:0.24 and 1.2 mg/kg
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Administration:Daily; oral
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Result:Decreased plasma aldosterone levels and reversed preexistent left ventricular interstitial fibrosis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 102676-87-9
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Appearance Solid
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분자량 223.27
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화학식 C14H13N3
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Color Light yellow to yellow
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SMILES
N#CC1=CC=C([C@H]2CCCC3=CN=CN23)C=C1
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Synonyms
(R)-Fadrozole; (R)-CGS 16949A free base; FAD286
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 110 mg/mL (492.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (12.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (12.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.4789 mL | 22.3944 mL | 44.7888 mL | 111.9720 mL |
| 5 mM | 0.8958 mL | 4.4789 mL | 8.9578 mL | 22.3944 mL | |
| 10 mM | 0.4479 mL | 2.2394 mL | 4.4789 mL | 11.1972 mL | |
| 15 mM | 0.2986 mL | 1.4930 mL | 2.9859 mL | 7.4648 mL | |
| 20 mM | 0.2239 mL | 1.1197 mL | 2.2394 mL | 5.5986 mL | |
| 25 mM | 0.1792 mL | 0.8958 mL | 1.7916 mL | 4.4789 mL | |
| 30 mM | 0.1493 mL | 0.7465 mL | 1.4930 mL | 3.7324 mL | |
| 40 mM | 0.1120 mL | 0.5599 mL | 1.1197 mL | 2.7993 mL | |
| 50 mM | 0.0896 mL | 0.4479 mL | 0.8958 mL | 2.2394 mL | |
| 60 mM | 0.0746 mL | 0.3732 mL | 0.7465 mL | 1.8662 mL | |
| 80 mM | 0.0560 mL | 0.2799 mL | 0.5599 mL | 1.3997 mL | |
| 100 mM | 0.0448 mL | 0.2239 mL | 0.4479 mL | 1.1197 mL |
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