| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
BRD5075 targets GPR65 (also known as TDAG8), a Galphas-coupled proton-sensing GPCR. It acts as a positive allosteric modulator, enhancing GPR65 activity under acidic conditions and promoting Galphas-dependent signaling pathways, including cAMP production and G protein recruitment.
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|---|---|
| ln Vitro |
In vitro, BRD5075 induces cAMP production in GPR65-expressing HeLa cells with EC50 values of 3.8 microM for wild-type GPR65 and 6.9 microM for the IBD risk variant GPR65 I231L. It reduces gene expression of pro-inflammatory cytokines including IL-1, IL-2, TNF, and chemokines, and decreases TNF-alpha secretion by GPR65 wild-type bone marrow-derived dendritic cells.
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| ln Vivo |
In vivo activity has been evaluated in rodent models of multiple sclerosis. BRD5075 administration demonstrates efficacy in a standard multiple sclerosis model, establishing that immune signaling can be modulated by targeting GPR65. The compound has potential for studying inflammatory bowel disease and other immune-mediated conditions.
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| Enzyme Assay |
For cAMP accumulation assays, HeLa cells overexpressing human GPR65 are lifted with Versene and suspended at 2.5 × 10⁵ cells/mL. Cells are incubated with BRD5075 (0-50 microM) at room temperature for 30 minutes. Eu-cAMP tracer is diluted 1:33 into detection buffer and added to assay wells. FRET emissions are read using a fluorescence plate reader.
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| Cell Assay |
For cytokine expression studies, GPR65 wild-type bone marrow-derived dendritic cells are treated with BRD5075 or DMSO control for 6 hours. RNA is extracted and gene expression levels of IL-1, IL-2, TNF, and chemokines are analyzed by qRT-PCR. TNF-alpha secretion in culture supernatants is measured by ELISA.
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| Animal Protocol |
For multiple sclerosis model studies, rodents are administered BRD5075 via appropriate route (oral or intraperitoneal). Efficacy is assessed by monitoring disease progression using clinical scoring systems. Immune cell infiltration in the central nervous system and cytokine profiles in serum and tissue homogenates are analyzed.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic parameters for BRD5075 are not fully published. As a small molecule PAM of GPR65, it is expected to have reasonable oral bioavailability. Solubility in DMSO is good. Further PK characterization including half-life, clearance, and tissue distribution requires additional studies.
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| Toxicity/Toxicokinetics |
Toxicity data for BRD5075 are limited. In preclinical studies, no substantial toxicity has been reported at efficacious doses. Standard safety pharmacology assessments including cardiovascular (hERG, blood pressure), CNS (Irwin test), and respiratory function would be required for therapeutic development.
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| References | |
| Additional Infomation |
BRD5075 is a research chemical probe for studying GPR65 biology. It has not received regulatory approval for any clinical indication. The compound is for research use only and is not for diagnostic or therapeutic applications. Potential applications include multiple sclerosis and inflammatory bowel disease research.
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| Molecular Formula |
C23H23N5O3
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|---|---|
| Molecular Weight |
417.46
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| Appearance |
Off-white to light yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~239.54 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO +40% PEG300 +5% Tween-80 +45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution。
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.99 mM) (saturation unknown) in 10% DMSO +90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution。 For example, if 1 mL of working solution is to be prepared, You can add 100 μL of the 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3954 mL | 11.9772 mL | 23.9544 mL | |
| 5 mM | 0.4791 mL | 2.3954 mL | 4.7909 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3954 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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