BRD5080
Based on 1 Customer Validation
BRD5080 is a GPR65 agonist. BRD5080 activates GPR65 to enhance the cAMP signaling pathway, reduce the expression of inflammatory cytokines and chemokines in dendritic cells, enhance the activity of human wild-type, mouse wild-type, and human GPR65I231L variant receptors in a pH-dependent manner, and mediate the recruitment of Gαs protein. BRD5080 can be used in the research of inflammatory bowel disease.
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- Purity: 99.44%
- 화학식: C24H23FN4O3
- 분자량:434.46
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보관:Powder -20°C, 3 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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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
BRD5080 enhances cAMP signaling in GPR65-expressing HeLa cells and reduces the expression of inflammatory cytokines and chemokines in mouse bone marrow-derived dendritic cells[1].
BRD5080 (1.56 μM; 30 min) specifically activates wild-type human GPR65 and wild-type murine GPR65 in HeLa cells, with no significant activity against human GPR4 or GPR68[2].
BRD5080 enhances pH-dependent cAMP production at concentrations ranging from 1.56 to 50 μM[2].
BRD5080 binds to both wild-type human GPR65 and wild-type murine GPR65 in Expi293F cells, and enhances the recruitment of Gαs protein at a concentration of 10 μM under pH-activated conditions[2].
BRD5080 (50 μM; 72 h) exerts no cytotoxic effect on HeLa cells expressing wild-type human GPR65[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells stably expressing wild-type human GPR65 (hGPR65)
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Concentration:50 μM
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Incubation Time:72 h
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Result:Showed no significant cytotoxicity to hGPR65-expressing HeLa cells over 72 hours.
Caused only a slight decrease in cell viability at the highest tested concentration of 50 μM.
Chemical Information
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Appearance Solid
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분자량 434.46
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화학식 C24H23FN4O3
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Color Off-white to light brown
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SMILES
O=C1C=C(C2=CC=C(COC(C)C)C=C2)NC3=C(C(NC4=C(F)C=C(C)C=C4)=O)C=NN31
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (230.17 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 (5.75 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 (5.75 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 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 (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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Handling Instructions (2659 KB)
References
[1]. Justus CR, et al. The Roles of Proton-Sensing G-Protein-Coupled Receptors in Inflammation and Cancer. Genes (Basel). 2024 Sep 1;15(9):1151. [Content Brief]
[2]. Neale I, et al. Small-molecule probe for IBD risk variant GPR65 I231L alters cytokine signaling networks through positive allosteric modulation. Science Advances. 2024;10(29):eadn2339. [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 | 2.3017 mL | 11.5085 mL | 23.0171 mL | 57.5427 mL |
| 5 mM | 0.4603 mL | 2.3017 mL | 4.6034 mL | 11.5085 mL | |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3017 mL | 5.7543 mL | |
| 15 mM | 0.1534 mL | 0.7672 mL | 1.5345 mL | 3.8362 mL | |
| 20 mM | 0.1151 mL | 0.5754 mL | 1.1509 mL | 2.8771 mL | |
| 25 mM | 0.0921 mL | 0.4603 mL | 0.9207 mL | 2.3017 mL | |
| 30 mM | 0.0767 mL | 0.3836 mL | 0.7672 mL | 1.9181 mL | |
| 40 mM | 0.0575 mL | 0.2877 mL | 0.5754 mL | 1.4386 mL | |
| 50 mM | 0.0460 mL | 0.2302 mL | 0.4603 mL | 1.1509 mL | |
| 60 mM | 0.0384 mL | 0.1918 mL | 0.3836 mL | 0.9590 mL | |
| 80 mM | 0.0288 mL | 0.1439 mL | 0.2877 mL | 0.7193 mL | |
| 100 mM | 0.0230 mL | 0.1151 mL | 0.2302 mL | 0.5754 mL |
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