| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
BP14979 selectively targets the dopamine D3 receptor (D3R). It acts as a partial agonist at this receptor, which belongs to the G protein-coupled receptor (GPCR) family and is primarily expressed in the limbic system. The compound exhibits high selectivity and affinity for D3 receptors over other dopamine receptor subtypes.
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| ln Vitro |
In cell-free receptor binding assays, BP14979 demonstrates high affinity for the dopamine D3 receptor. The compound's structural characteristics enable it to modulate D3 receptor efficacy. Its design is based on differences in efficacy compared with D3R-selective antagonists, providing opportunities for optimizing new drug development.
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| ln Vivo |
In cellular models, BP14979 acts as a D3R-selective partial agonist, modulating dopaminergic signaling pathways. The compound has shown activity in studies of neurological diseases. It can be used to develop ligands with higher selectivity and affinity for D3 receptors. Detailed cellular assay data are described in the primary literature.
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| Enzyme Assay |
The in vitro receptor binding assay for BP14979 typically involves incubating membrane preparations from cells expressing dopamine D3 receptors with radiolabeled ligands and varying concentrations of the compound. Competition binding curves are generated to calculate Ki values. The compound's partial agonist activity is assessed in functional assays measuring receptor-mediated signaling such as cAMP inhibition or β-arrestin recruitment.
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| Cell Assay |
Cells expressing dopamine D3 receptors are cultured and treated with BP14979 at concentrations ranging from 0.1 nM to 10 µM. Receptor-mediated signaling is assessed by measuring cAMP levels, calcium mobilization, or other downstream signaling events. EC₅₀ values for receptor activation are determined from dose-response curves. Cell viability is monitored to ensure compound concentrations are not cytotoxic.
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| Animal Protocol |
In vivo studies have been conducted in animal models of binge-eating disorder, OCD, RLS, and nicotine addiction. BP14979 is typically administered orally. Endpoints include assessment of compulsive behavior, motor function, and reward-related behaviors. The compound is in clinical trial NCT01785147 for smoking cessation.
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| ADME/Pharmacokinetics |
BP14979 (C₂₃H₃₄N₄O₂, MW 398.54, CAS 1000036-77-0) is a small molecule compound. It is soluble in DMSO. The compound is typically stored as a powder at -20°C. In vivo pharmacokinetic parameters including oral bioavailability, half-life, and Cmax have been characterized in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for BP14979 are being evaluated as part of its clinical development program. The compound is for research use only and is not yet approved for clinical use. Clinical trial safety data are being collected in ongoing studies.
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| Additional Infomation |
BP14979 (also known as BP-14979, BP1,4979, and BP 1,4979) is a D3R-selective partial agonist under clinical investigation. It is being studied for binge-eating disorder, OCD, RLS, and smoking withdrawal. The compound is in clinical trial NCT01785147.
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| Exact Mass |
398.2682
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|---|---|
| CAS # |
1000036-77-0
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| PubChem CID |
57964460
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
29
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| Complexity |
544
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| Defined Atom Stereocenter Count |
0
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| Synonyms |
BP14979 BP-14979 BP 14979
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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