BMS-564929
Based on 6 publication(s) in Google Scholar
BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a Ki of 2.11±0.16 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.28%
- CAS. Nr.: 627530-84-1
- Formel: C14H12ClN3O3
- Molecular Weight:305.72
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) BMS-564929
More- Redox Biol. 2025 Jul 31:86:103793. [Abstract]
- Food Chem. 2019 Sep 24;4:100056. [Abstract]
- Cancers (Basel). 2023 Oct 15;15(20):4995. [Abstract]
- J Chromatogr A. 2019 Aug 30:1600:183-196. [Abstract]
- Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2020 Aug;37(8):1253-1263. [Abstract]
- MethodsX. 2020 May 21;7:100926. [Abstract]
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RT-PCR
Biologische Aktivität
Ki: 2.11±0.16 nM (Androgen receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C2C12 | EC50 |
0.44 nM
Compound: 2
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Agonist activity at androgen receptor in mouse C2C12 cells by receptor transactivation assay
Agonist activity at androgen receptor in mouse C2C12 cells by receptor transactivation assay
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[PMID: 17574413] |
| C2C12 | EC50 |
0.7 nM
Compound: 3
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Agonist activity at androgen receptor expressed in C2C12 mouse cells by luciferase reporter transactivation assay
Agonist activity at androgen receptor expressed in C2C12 mouse cells by luciferase reporter transactivation assay
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[PMID: 17552509] |
| C2C12 | EC50 |
7.8 nM
Compound: 1
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Agonist activity at rat androgen receptor expressed in mouse skeletal muscle C2C12 cells assessed as transcriptional activation after 24 hrs by androgen-specific response element driven luciferase reporter gene assay
Agonist activity at rat androgen receptor expressed in mouse skeletal muscle C2C12 cells assessed as transcriptional activation after 24 hrs by androgen-specific response element driven luciferase reporter gene assay
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[PMID: 19351168] |
BMS-564929 exhibits a potency (EC50, calculated as the concentration at which 50% of the maximum stimulatory effect of DHT is achieved) of 0.44±0.03 nM in the C2C12 myoblast cell line. In the PEC cell line, the EC50 for BMS-564929 is 8.66±0.22 nM. BMS-564929 is more than 1000-fold selective for AR vs. estrogen receptors (ER) α and β, glucocorticoid receptor (GR), and mineralocorticoid receptor (MR), and approximately 400-fold selective vs. progesterone receptor (PR). BMS-564929 shows no measurable activity in functional transactivation assays with ERα/β, GR, MR, or PR at concentrations up to 30 μM[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.
Chemical Information
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CAS. Nr. 627530-84-1
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Appearance Solid
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Molecular Weight 305.72
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Formel C14H12ClN3O3
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Color White to off-white
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SMILES
N#CC1=CC=C(N(C(N2[C@@]3([H])[C@H](O)CC2)=O)C3=O)C(C)=C1Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Redox Biol
Arylsulfatase K attenuates airway epithelial cell senescence in COPD by regulating parkin-mediated mitophagy. [Abstract]2025 Jul 31:86:103793. PMID: 40763656
BMS-564929 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jul 31:86:103793. [Abstract]
Relative ARSK mRNA levels with or without the treatment of BMS-564929 (AR agonist) (20 nM) in HBE cells.
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Food Chem
Monitoring of selective androgen receptor modulators in bovine muscle tissue by ultra-high performance liquid chromatography-tandem mass spectrometry. [Abstract]2019 Sep 24;4:100056. PMID: 31650129 -
Cancers (Basel)
A Combinatorial Regulatory Platform Determines Expression of RNA Polymerase III Subunit RPC7α (POLR3G) in Cancer. [Abstract]2023 Oct 15;15(20):4995. PMID: 37894362 -
J Chromatogr A
Development and validation of a semi-quantitative ultra-high performance liquid chromatography-tandem mass spectrometry method for screening of selective androgen receptor modulators in urine. [Abstract]2019 Aug 30:1600:183-196. PMID: 31053351 -
Food Addit Contam Part A Chem Anal Control Expo Risk Assess
2020 Aug;37(8):1253-1263. PMID: 32401172 -
MethodsX
Enhanced UHPLC-MS/MS screening of selective androgen receptor modulators following urine hydrolysis. [Abstract]2020 May 21;7:100926. PMID: 32547930
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (163.55 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (8.18 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.
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.
Protokoll
The human cancer epithelial breast cell lines MDA MB-453 and T47D, which endogenously express AR and progesterone receptor (PR), respectively, are used for radioligand competition binding assays. Binding assays are conducted by incubating BMS-564929 at various concentrations with either [3H]DHT or [3H]progesterone with the cells for 2 h at room temperature. For ERα and ERβ, fusion proteins expressed in Escherichia coli, consisting of maltose binding protein, a specific biotinylation sequence, an enterokinase cleavage site, and either the ERα or ERβ LBD is used. Binding reactions are conducted by incubating ERα and ERβ LBD with BMS-564929 and [3H]E2 for 2 h at room temperature. Specific binding activity to the mineralocorticoid receptor (MR) by BMS-564929 is evaluated by competition binding assay using kidney cytosolic preparations and [3H]aldosterone. The kidneys are obtained from adrenalectomized rats to remove the endogenous source of aldosterone and to increase the MR concentration in the cytosol of kidney cells. Binding reactions are incubated for 2 h on ice in the presence of excess mifepristone (RU486) to block nonspecific glucocorticoid receptor (GR) binding. A fluorescence polarization based assay is used for GR binding, as per manufacturer recommendations. Inhibitory constants (Ki, app) defining apparent binding affinity of test compounds to intracellular receptors are calculated from the observed inhibition of natural ligand binding at multiple concentrations of test compound. SHBG binding is performed using a standard charcoal assay. Reagents: 1 mg lyophilized SHGB powder (Tris), [3H]DHT, 3% charcoal, and 0.4% Dextran in PBS; binding buffer: 50 mM Tris, pH 7.6, 100 mM NaCl, 1 mM EDTA, 1 mM DTT, and mock lysate (3.5 μg/100 μL buffer); stock solutions: stock SHBG protein: 1 mg/mL in water=20 μM; stock [3H]DHT ligand: 9 μM; DHT: 10 mM in DMSO; BMS 564929: 10 mM in DMSO. Compounds diluted in binding buffer are added to 40 nM [3H]DHT and 20 nM SHBG protein in 200 μL volume and incubated for 1 h at room temperature. Total binding: 40 nM [3H]DHT and 20 nM SHBG protein in 200 μL volume; nonspecific binding: 40 nM [3H]DHT and 20 nM SHBG protein and 1 mM cold DHT in 200 μL volume. At the end of the incubation period, 200 μL of the charcoal solution (3% containing 0.04% dextran) is added to 200 μL of the reactions and shaken for 15 min before centrifugation. Supernatant (200 μL) is then transferred to the wells of a 24-well white Optiplate; 200 μL of scintillant are added with mixing. Radioactivity counts are read in Topcount[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Matched sets of castrated, sexually mature Harlan Sprague Dawley rats (42-56 d old, 200-250 g) are dosed once daily by oral gavage with BMS-564929 (0.00001-10 mg/kg) in solution/suspension of 80% PEG 400 and 20% Tween 20 for 14 d. Two control groups, one sham operated intact and one castrated, are dosed orally with the PEG/TW vehicle only, beginning on d 15 after surgery. Animals are dosed (vol/wt) at 1 mL/kg body weight. T propionate (TP) is dosed once daily sc in a 10% ethanol/90% peanut oil vehicle as a reference compound (0.03-10 mg/kg). After 14 d of treatment, the animals are killed by carbon dioxide asphyxiation, the levator ani and the ventral prostate are surgically removed and weighed, and serum is collected for LH measurements.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.2710 mL | 16.3548 mL | 32.7097 mL | 81.7742 mL |
| 5 mM | 0.6542 mL | 3.2710 mL | 6.5419 mL | 16.3548 mL | |
| 10 mM | 0.3271 mL | 1.6355 mL | 3.2710 mL | 8.1774 mL | |
| 15 mM | 0.2181 mL | 1.0903 mL | 2.1806 mL | 5.4516 mL | |
| 20 mM | 0.1635 mL | 0.8177 mL | 1.6355 mL | 4.0887 mL | |
| 25 mM | 0.1308 mL | 0.6542 mL | 1.3084 mL | 3.2710 mL | |
| 30 mM | 0.1090 mL | 0.5452 mL | 1.0903 mL | 2.7258 mL | |
| 40 mM | 0.0818 mL | 0.4089 mL | 0.8177 mL | 2.0444 mL | |
| 50 mM | 0.0654 mL | 0.3271 mL | 0.6542 mL | 1.6355 mL | |
| 60 mM | 0.0545 mL | 0.2726 mL | 0.5452 mL | 1.3629 mL | |
| 80 mM | 0.0409 mL | 0.2044 mL | 0.4089 mL | 1.0222 mL | |
| 100 mM | 0.0327 mL | 0.1635 mL | 0.3271 mL | 0.8177 mL |
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