BAY-298
Based on 1 Customer Validation
BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels.
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- Pureté: 99.96%
- CAS No.: 2471978-97-7
- Formule: C27H21ClFN3O2
- Masse moléculaire:473.93
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
IC50: 185 nM (hLH), 46nM (rLH) and 78 nM (cLH)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
3 μM
Compound: 33; BAY-298
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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] |
| HEK293 | IC50 |
78 nM
Compound: 33; BAY-298
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Antagonist activity at cynomolgus monkey luteinizing hormone receptor expressed in HEK293 cells assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition and measured after 30 mins by cell base
Antagonist activity at cynomolgus monkey luteinizing hormone receptor expressed in HEK293 cells assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition and measured after 30 mins by cell base
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[PMID: 31670515] |
BAY-298 (iv of 0.5 mg/kg or po of 2 mg/kg) has t1/2s of 31 hours and 33 hours for iv and po. And the Cmaxs are 0.28 kg/L and 0.066 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:4.5, 9, 18, 36, 72 mg/kg
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Administration:Oral; for 8 days
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Result:Dosedependently lowered serum estradiol levels in proestrus.
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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 31 hours and 33 hours for iv and po. And the Cmaxs are 0.28 kg/L and 0.066 kg/L for iv and po.
Chemical Information
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CAS No. 2471978-97-7
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Appearance Solid
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Masse moléculaire 473.93
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Formule C27H21ClFN3O2
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Color Off-white to light yellow
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SMILES
O=C(N1[C@@H](C2=CC=C(Cl)C=C2)C3=C(N=CC=C3)CC1)NC4=CC=C(OC5=CC=C(F)C=C5)C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (211.00 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.
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.
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 | 2.1100 mL | 10.5501 mL | 21.1002 mL | 52.7504 mL |
| 5 mM | 0.4220 mL | 2.1100 mL | 4.2200 mL | 10.5501 mL | |
| 10 mM | 0.2110 mL | 1.0550 mL | 2.1100 mL | 5.2750 mL | |
| 15 mM | 0.1407 mL | 0.7033 mL | 1.4067 mL | 3.5167 mL | |
| 20 mM | 0.1055 mL | 0.5275 mL | 1.0550 mL | 2.6375 mL | |
| 25 mM | 0.0844 mL | 0.4220 mL | 0.8440 mL | 2.1100 mL | |
| 30 mM | 0.0703 mL | 0.3517 mL | 0.7033 mL | 1.7583 mL | |
| 40 mM | 0.0528 mL | 0.2638 mL | 0.5275 mL | 1.3188 mL | |
| 50 mM | 0.0422 mL | 0.2110 mL | 0.4220 mL | 1.0550 mL | |
| 60 mM | 0.0352 mL | 0.1758 mL | 0.3517 mL | 0.8792 mL | |
| 80 mM | 0.0264 mL | 0.1319 mL | 0.2638 mL | 0.6594 mL | |
| 100 mM | 0.0211 mL | 0.1055 mL | 0.2110 mL | 0.5275 mL |
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