Bevurogant
Based on 1 Customer Validation
Bevurogant (BI 730357) is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.54%
- No. CAS: 1817773-66-2
- Fòrmula: C26H28N8O3S
- Peso molecular:532.62
-
Almacenamiento: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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Small Molecule Immuno-Oncology Compound Library
HY-L031
-
Drug Repurposing Compound Library
HY-L035
-
Transcription Factor-Targeted Library
HY-L090
-
Nuclear Receptor Compound Library
HY-L126
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
Bevurogant can target the Th17 cell-associated pathway, potently inhibit P-gp and potentially inhibit BCRP, and is applicable for investigating Th17-mediated inflammatory diseases such as psoriasis[2].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 1817773-66-2
-
Appearance Solid
-
Peso molecular 532.62
-
Fòrmula C26H28N8O3S
-
Color White to light yellow
-
SMILES
C[C@@H](C1CC1)N2C3=NC(C4=C(C)N=CN=C4C5CC5)=NC=C3N=C(C2=O)NCC6=CC=C(C=N6)S(C)(=O)=O
-
Synonyms
BI 730357
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (469.38 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: ≥ 2.08 mg/mL (3.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Ficha de datos (274 KB)
-
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. BAKONYI J, et, al. Compounds as modulators of ror gamma. US20150291607A1.
[2]. Choi H, et al. The Effect of BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma t Antagonist, Bevurogant) on the Pharmacokinetics of a Transporter Probe Cocktail, Including Digoxin, Furosemide, Metformin, and Rosuvastatin: An Open-Label, Non-randomized, 2-Period Fixed-Sequence Trial in Healthy Subjects. Clin Pharmacol Drug Dev. 2024 Feb;13(2):197-207. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8775 mL | 9.3876 mL | 18.7751 mL | 46.9378 mL |
| 5 mM | 0.3755 mL | 1.8775 mL | 3.7550 mL | 9.3876 mL | |
| 10 mM | 0.1878 mL | 0.9388 mL | 1.8775 mL | 4.6938 mL | |
| 15 mM | 0.1252 mL | 0.6258 mL | 1.2517 mL | 3.1292 mL | |
| 20 mM | 0.0939 mL | 0.4694 mL | 0.9388 mL | 2.3469 mL | |
| 25 mM | 0.0751 mL | 0.3755 mL | 0.7510 mL | 1.8775 mL | |
| 30 mM | 0.0626 mL | 0.3129 mL | 0.6258 mL | 1.5646 mL | |
| 40 mM | 0.0469 mL | 0.2347 mL | 0.4694 mL | 1.1734 mL | |
| 50 mM | 0.0376 mL | 0.1878 mL | 0.3755 mL | 0.9388 mL | |
| 60 mM | 0.0313 mL | 0.1565 mL | 0.3129 mL | 0.7823 mL | |
| 80 mM | 0.0235 mL | 0.1173 mL | 0.2347 mL | 0.5867 mL | |
| 100 mM | 0.0188 mL | 0.0939 mL | 0.1878 mL | 0.4694 mL |
Bevurogant Related Classifications
HY-132810 Related Classifications
Powered by Bioz