| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
SB269652 targets the dopamine D2 receptor (D2R) and D3 receptor (D3R) as a negative allosteric modulator. It acts by binding in a bitopic manner at one protomer of a D2R dimer and modulating the binding of dopamine at a second protomer. This unique mechanism differentiates D2R monomers from dimers or oligomers.
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| ln Vitro |
In vitro, SB269652 potently abolished specific binding of [³H]nemonapride and [³H]spiperone to transfected D3 receptors when radioligands were used at 0.2 and 0.5 nM, respectively. It demonstrates potent activity in receptor binding assays, confirming its role as a negative allosteric modulator with high affinity for its target receptors.
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| ln Vivo |
In vivo, SB269652 has been studied for its potential therapeutic applications in neuropsychiatric disorders such as schizophrenia and drug addiction. By selectively modulating dopamine receptor function, it provides insights into receptor dimerization and signaling pathways. It represents a next-generation dopaminergic therapeutic with improved specificity.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay typically involves competition binding experiments using radiolabeled ligands such as [³H]nemonapride or [³H]spiperone. Membranes from cells expressing D2 or D3 receptors are incubated with varying concentrations of SB269652 and a fixed concentration of radioligand. Nonspecific binding is determined in the presence of excess unlabeled ligand. Bound radioactivity is measured after filtration and washing.
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| Cell Assay |
In vitro cell-based assays are performed using Chinese hamster ovary (CHO) cells transfected with D2 or D3 receptors. Cells are cultured in appropriate media and treated with SB269652 at various concentrations. Functional assays such as inhibition of forskolin-stimulated cAMP accumulation or β-arrestin recruitment are conducted to assess receptor modulation. Data are analyzed to determine IC₅₀ values.
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| Animal Protocol |
In vivo animal experiments for SB269652 typically involve rodent models of neuropsychiatric disorders. Animals are administered SB269652 via routes such as intraperitoneal injection or oral gavage. Behavioral tests, including locomotor activity, prepulse inhibition, and drug-induced hyperlocomotion, are performed to assess the compound's effects on dopamine-mediated behaviors. Brain and plasma samples are collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of SB269652 have been characterized in preclinical species. It shows suitable drug-like properties for central nervous system penetration. The compound is typically formulated in suitable vehicles for in vivo administration. Detailed PK parameters such as half-life, clearance, volume of distribution, and oral bioavailability are determined from plasma concentration-time profiles following intravenous and oral dosing.
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| Toxicity/Toxicokinetics |
Toxicological data for SB269652 are limited as it is primarily a research tool compound. In standard preclinical safety assessments, it is expected to be evaluated for potential off-target effects and general toxicity in rodent and non-rodent species. The compound is intended for research use only and not for therapeutic use in humans.
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| References | |
| Additional Infomation |
SB269652 is a novel chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology. It is the first drug-like allosteric modulator of the dopamine D2 receptor. Its discovery has contributed to the development of next-generation dopaminergic therapeutics with improved specificity. It has not been approved for clinical use and remains an investigational research compound.
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| Molecular Formula |
C27H30N4O
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|---|---|
| Molecular Weight |
426.5533
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| Exact Mass |
426.241
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| CAS # |
215802-15-6
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| PubChem CID |
9910352
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
690.6±55.0 °C at 760 mmHg
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| Flash Point |
371.5±31.5 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.662
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| LogP |
5.11
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
693
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CC2=C(C=CC=C2)N1)N[C@H]3CC[C@H](CCN(CC4)CC5=C4C=CC(C#N)=C5)CC3
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| InChi Key |
JGLGOAQPUQITLD-OGAOHHHESA-N
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| InChi Code |
InChI=1S/C27H30N4O/c28-17-20-5-8-21-12-14-31(18-23(21)15-20)13-11-19-6-9-24(10-7-19)29-27(32)26-16-22-3-1-2-4-25(22)30-26/h1-5,8,15-16,19,24,30H,6-7,9-14,18H2,(H,29,32)/t19-,24-
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| Chemical Name |
N-((1r,4r)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide
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| Synonyms |
SB269652; SB-269652; SB2 69652; SB269,652; SB-269,652; SB 269,652.
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3444 mL | 11.7220 mL | 23.4439 mL | |
| 5 mM | 0.4689 mL | 2.3444 mL | 4.6888 mL | |
| 10 mM | 0.2344 mL | 1.1722 mL | 2.3444 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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