RU 59063
Based on 1 Customer Validation
RU 59063 is a high-affinity, selective nonsteroidal androgen receptor (AR) ligand that acts as a partial AR agonist/antagonist in CV-1 cell transcription assays. RU 59063 has a Ka value of 6.2×109 M-1 for human AR. RU 59063 induces a conformation of AR that can bind to the androgen response element (ARE), triggers partial AR-dependent transcriptional activation, and antagonizes testosterone-induced AR transcriptional activity. RU 59063 inhibits testosterone propionate-induced ornithine decarboxylase activity in mouse kidneys and testosterone propionate-induced prostate weight gain in rats. RU 59063 can be used in studies related to prostate cancer.
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- Purity: 98.61%
- CAS No.: 155180-53-3
- 화학식: C17H18F3N3O2S
- 분자량:385.40
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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hAR |
RU 59063 (0.1-20 nM; 24 h at 0°C) binds to full-length and truncated human androgen receptors expressed in COS-1 cells, with the same number of binding sites as testosterone. Its Ka value is 6×109 M-1, which is 8 times the Ka value of testosterone binding to the full-length human androgen receptor[2].
RU 59063 (1-25000 nM; 24 h) competes with [3H]testosterone for binding to rat prostate AR in a concentration-dependent manner, with a relative binding affinity (RBA) of 300, where the RBA of testosterone is defined as 100[2].
RU 59063 (1 μM; 30 h) fully promotes the binding of androgen receptor (rARD46-408G12C mutant) to androgen response elements in CV-1 cells, reduces the activity of the pCMV-ARE2-CAT reporter gene to 42.5% of that in the control group, and exerts an effect comparable to that of 10 nM testosterone[1].
RU 59063 (1 μM; 30 h) acts as a partial agonist/antagonist of wild-type rat androgen receptor in CV-1 cells, inducing 35% of the transcriptional activation activity elicited by 10 nM testosterone and reducing testosterone-induced activation activity by 34%-61%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice (male, ~30 g, castrated and challenged with testosterone propionate)[2]
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Dosage:1.7 mg/kg (subcutaneous inhibition); 1 mg/kg (subcutaneous inhibition); 1 mg/kg (oral no inhibition)
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Administration:s.c.; single dose; p.o.; single dose
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Result:Inhibited the TP-induced renal ODC activity by 64%.
Inhibited the TP-induced renal ODC activity by 58%.
Did not inhibit the TP-induced renal ODC activity (0% inhibition).
Chemical Information
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CAS No. 155180-53-3
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Appearance Solid
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분자량 385.40
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화학식 C17H18F3N3O2S
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Color White to off-white
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SMILES
N#CC1=CC=C(C=C1C(F)(F)F)N(C2=O)C(N(C2(C)C)CCCCO)=S
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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 : 100 mg/mL (259.47 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: ≥ 2.5 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (6.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (275 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
[2]. Teutsch G, et al. Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor. The Journal of steroid biochemistry and molecular biology. 1994 Jan;48(1):111-9. [Content Brief]
[3]. Gim HJ, et al. Conformational dynamics of androgen receptors bound to agonists and antagonists. Scientific reports. 2021 Aug 05;11(1):15887. [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 | 2.5947 mL | 12.9735 mL | 25.9471 mL | 64.8677 mL |
| 5 mM | 0.5189 mL | 2.5947 mL | 5.1894 mL | 12.9735 mL | |
| 10 mM | 0.2595 mL | 1.2974 mL | 2.5947 mL | 6.4868 mL | |
| 15 mM | 0.1730 mL | 0.8649 mL | 1.7298 mL | 4.3245 mL | |
| 20 mM | 0.1297 mL | 0.6487 mL | 1.2974 mL | 3.2434 mL | |
| 25 mM | 0.1038 mL | 0.5189 mL | 1.0379 mL | 2.5947 mL | |
| 30 mM | 0.0865 mL | 0.4325 mL | 0.8649 mL | 2.1623 mL | |
| 40 mM | 0.0649 mL | 0.3243 mL | 0.6487 mL | 1.6217 mL | |
| 50 mM | 0.0519 mL | 0.2595 mL | 0.5189 mL | 1.2974 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4325 mL | 1.0811 mL | |
| 80 mM | 0.0324 mL | 0.1622 mL | 0.3243 mL | 0.8108 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2595 mL | 0.6487 mL |
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