BRD5075
Based on 1 Customer Validation
BRD5075 is a selective GPR65 activator. BRD5075 enhances GPR65 activity under acidic conditions, promotes Gαs-dependent signaling pathways, including cAMP production and G protein recruitment. BRD5075 regulates the cytokine and chemokine expression network in dendritic cells, and inhibits the expression of pro-inflammatory cytokines and chemokines in a GPR65-dependent manner. BRD5075 is applicable to research related to inflammatory bowel disease.
For research use only. We do not sell to patients.
- Purity : 98.72%
- Formula: C23H23N5O3
- Molecular Weight:417.46
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
BRD5075 (1.56-50 μM; 30 min) potently and specifically induces cAMP production in HeLa cells via positive allosteric modulation of wild-type hGPR65 and mGPR65, with no activity against the related pH-sensing receptors hGPR4 or hGPR68[1].
BRD5075 (5-20 μM; 3 hours) inhibits LPS (HY-D1056)-induced TNF secretion in human MDDCs under pH 6.6 conditions[1].
BRD5075 (1.56-50 μM; 72 hours) shows no cytotoxicity against hGPR65-expressing HeLa cells at concentrations up to 25 μM, and only exhibits extremely low cytotoxicity at 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HeLa cells stably expressing wild-type hGPR65
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Concentration:1.56, 3.125, 6.25, 12.5, 25 and 50 μM
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Incubation Time:72 hours
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Result:Was not cytotoxic to hGPR65-expressing HeLa cells over 72 hours, with only a slight decrease in cell viability observed at 50 μM.
Chemical Information
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Appearance Solid
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Molecular Weight 417.46
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Formula C23H23N5O3
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Color Off-white to light yellow
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SMILES
O=C1C=C(C2=CC=C(COC(C)C)C=C2)NC3=C(C(NC4=NC=C(C)C=C4)=O)C=NN31
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (239.54 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)
In Vivo:
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 (5.99 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.
In Vivo Dissolution Calculator
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.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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LPS-Induced Endotoxemia/Systemic Inflammation
Lipopolysaccharide (LPS)-induced endotoxemia is a widely used in vivo model of acute systemic inflammation in which LPS, a Gram-negative bacterial endotoxin, activates innate immune signaling primarily through TLR4, leading to rapid and transient induction of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β in circulation and tissues. This cytokine surge is commonly used as a measurable readout of systemic inflammatory activation and immune dysregulation, and is typically assessed within hours after intraperitoneal LPS administration in mouse models of endotoxemia. The model captures key features of systemic inflammatory response syndrome, including cytokine release, immune cell activation, and downstream tissue responses, and has been used to evaluate anti-inflammatory interventions such as cytokine modulation, lipid mediators, and immune cell-targeting therapies.
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DSS-Induced Colitis
Dextran sulfate sodium (DSS)-induced colitis is generated by administering DSS in mouse drinking water, producing epithelial injury, barrier disruption, weight loss, diarrhea, fecal blood, colon shortening, histologic mucosal damage, and inflammatory mediator changes; the model is mainly used to study acute or chronic intestinal inflammation resembling selected features of ulcerative colitis. DSS injury is interpreted through clinical and tissue readouts rather than a single molecular endpoint: daily body weight, stool consistency, and bleeding are combined into a disease activity index, while colon length, histology, cytokines, myeloperoxidase activity, intestinal permeability, and tight-junction markers provide complementary measures of inflammation and barrier damage.
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TNBS-Induced Colitis
TNBS-induced colitis is produced by intrarectal delivery of 2,4,6-trinitrobenzene sulfonic acid in ethanol, where ethanol disrupts the mucosal barrier and TNBS haptenates colonic proteins, generating immune-mediated colonic inflammation with weight loss, diarrhea, ulceration, transmural injury, inflammatory-cell infiltration, and cytokine responses. The model is used as an experimental intestinal inflammation model with Crohn’s disease–like features, especially when Th1-type responses, IL-12–dependent inflammation, chronic relapsing inflammation, or fibrosis-related endpoints are studied.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Monocyte-derived dendritic cell differentiation
Human monocyte-derived dendritic cells are generated by isolating PBMC-derived monocytes and culturing them with GM-CSF plus IL-4, which produces cells with dendritic-cell antigen-presenting properties, reduced monocyte phenotype, and increased dendritic-cell functional readouts such as antigen uptake, allogeneic T-cell stimulation, and expression of markers including HLA-DR, CD80, CD86, CD83, CD1a, or CD209 depending on protocol and maturation state. The main readout is phenotypic and functional differentiation: immature MoDCs are commonly evaluated by loss or reduction of CD14 with acquisition of dendritic-cell markers and antigen uptake capacity, whereas mature MoDCs are evaluated by increased CD83, CD80, CD86, HLA-DR, and T-cell stimulatory function after exposure to maturation stimuli such as TNF-α or a cytokine/PGE2 cocktail.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 2.3954 mL | 11.9772 mL | 23.9544 mL | 59.8860 mL |
| 5 mM | 0.4791 mL | 2.3954 mL | 4.7909 mL | 11.9772 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3954 mL | 5.9886 mL | |
| 15 mM | 0.1597 mL | 0.7985 mL | 1.5970 mL | 3.9924 mL | |
| 20 mM | 0.1198 mL | 0.5989 mL | 1.1977 mL | 2.9943 mL | |
| 25 mM | 0.0958 mL | 0.4791 mL | 0.9582 mL | 2.3954 mL | |
| 30 mM | 0.0798 mL | 0.3992 mL | 0.7985 mL | 1.9962 mL | |
| 40 mM | 0.0599 mL | 0.2994 mL | 0.5989 mL | 1.4971 mL | |
| 50 mM | 0.0479 mL | 0.2395 mL | 0.4791 mL | 1.1977 mL | |
| 60 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9981 mL | |
| 80 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7486 mL | |
| 100 mM | 0.0240 mL | 0.1198 mL | 0.2395 mL | 0.5989 mL |
BRD5075 Related Classifications
HY-162734 Related Classifications
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