BAY-899
Based on 1 publication(s) in Google Scholar
BAY-899, a chemical probe, is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.93%
- No. CAS: 2471967-92-5
- Fòrmula: C25H19F2N5O2
- Peso molecular:459.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) BAY-899
More
Actividad biológica
IC50: 185 nM (hLH) and 46nM (rLH)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
10.6 μM
Compound: 36; BAY-899
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Inhibition of human ERG expressed in HEK293 cells at holding potential -80 mV by whole-cell voltage-clamp method
Inhibition of human ERG expressed in HEK293 cells at holding potential -80 mV by whole-cell voltage-clamp method
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[PMID: 31670515] |
BAY-899 (iv of 0.5 mg/kg or po of 2 mg/kg) has a t1/2 of 11 hours and 12 hours for iv and po. And the Cmax is 0.97 kg/L and 0.24 kg/L for iv and po[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Intact female rats[1]
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Dosage:12.5 mg/kg
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Administration:Oral; for 8 days
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Result:Showed an efficiency to reduce serum estradiol levels.
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Animal Model:Female and male Wistar rats[1]
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Dosage:0.5 mg/kg of iv or 2 mg/kg of po
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Administration:Iv or po
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Result:Has t1/2s of 11 hours and 12 hours for iv and po. And the Cmaxs are 0.97 kg/L and 0.24 kg/L for iv and po.
Chemical Information
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No. CAS 2471967-92-5
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Appearance Solid
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Peso molecular 459.45
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Fòrmula C25H19F2N5O2
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Color White to off-white
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SMILES
O=C(N1[C@@H](C2=CC=C(F)C=C2)C3=C(N=CC=C3)CC1)NC4=CN=C(OC5=CC=C(F)C=C5)N=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175
Solvente y solubilidad
DMSO : 100 mg/mL (217.65 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: ≥ 3.5 mg/mL (7.62 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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: ≥ 3.5 mg/mL (7.62 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1765 mL | 10.8826 mL | 21.7652 mL | 54.4129 mL |
| 5 mM | 0.4353 mL | 2.1765 mL | 4.3530 mL | 10.8826 mL | |
| 10 mM | 0.2177 mL | 1.0883 mL | 2.1765 mL | 5.4413 mL | |
| 15 mM | 0.1451 mL | 0.7255 mL | 1.4510 mL | 3.6275 mL | |
| 20 mM | 0.1088 mL | 0.5441 mL | 1.0883 mL | 2.7206 mL | |
| 25 mM | 0.0871 mL | 0.4353 mL | 0.8706 mL | 2.1765 mL | |
| 30 mM | 0.0726 mL | 0.3628 mL | 0.7255 mL | 1.8138 mL | |
| 40 mM | 0.0544 mL | 0.2721 mL | 0.5441 mL | 1.3603 mL | |
| 50 mM | 0.0435 mL | 0.2177 mL | 0.4353 mL | 1.0883 mL | |
| 60 mM | 0.0363 mL | 0.1814 mL | 0.3628 mL | 0.9069 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2721 mL | 0.6802 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2177 mL | 0.5441 mL |
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