| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
FAUC-365 selectively targets the dopamine D3 receptor with a Ki value of 0.5 nM, demonstrating exceptionally high binding affinity. It exhibits significantly lower binding affinities at other dopamine receptor subtypes, with Ki values of 340 nM at D4.4, 2600 nM at D2short, and 3600 nM at D2Long receptors. This represents over 100-fold selectivity for D3 over D2 and D4 receptors. FAUC-365's mechanism of action is as a potent and selective antagonist, blocking dopamine-mediated signaling at the D3 receptor.
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| ln Vitro |
FAUC-365 demonstrates potent antagonist activity at the dopamine D3 receptor with a Ki of 0.5 nM in radioligand binding assays. It shows remarkable selectivity, with Ki values of 340 nM, 2600 nM, and 3600 nM for D4.4, D2short, and D2Long receptors, respectively. This high selectivity makes FAUC-365 a valuable tool for studying D3 receptor function in neuropharmacology. The compound's activity profile is consistent with its classification as a highly selective D3 receptor antagonist.
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| ln Vivo |
FAUC-365 is used in vivo to investigate D3 receptor function in animal models of neuropsychiatric disorders. It has potential applications in the study of schizophrenia and Parkinson's disease, where the D3 receptor is implicated in the pathophysiology and treatment response. The compound's high selectivity for D3 over D2 receptors suggests a reduced potential for extrapyramidal side effects, making it a valuable tool for differentiating D3-mediated effects from those mediated by D2 receptors in vivo.
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| Enzyme Assay |
Non-cellular receptor binding assays for FAUC-365 are performed using competitive radioligand binding displacement studies. Membrane preparations from cells expressing recombinant human dopamine receptors (D2short, D2Long, D3, and D4.4) are incubated with a radiolabeled D3-selective ligand (e.g., [³H]7-OH-DPAT or [¹²⁵I]iodosulpride) and varying concentrations of FAUC-365. After incubation, the mixture is filtered through glass fiber filters to separate bound from free radioligand, and the retained radioactivity is measured by scintillation counting. IC50 values are determined from displacement curves, and Ki values are calculated using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cellular assays for FAUC-365 involve treating cells expressing the human dopamine D3 receptor with the compound to assess its functional antagonist activity. Typically, cells are pre-incubated with FAUC-365 at various concentrations, followed by stimulation with a D3 receptor agonist (e.g., dopamine or quinpirole). The inhibition of agonist-induced signaling, measured as the reduction in cAMP accumulation (as D3 receptors are coupled to Gi proteins), is quantified using a cAMP ELISA or HTRF-based assay. The IC50 for antagonism is determined from dose-response curves to confirm the compound's antagonist properties.
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| Animal Protocol |
In vivo animal experiments with FAUC-365 are conducted in rodent models of neuropsychiatric disorders to assess D3 receptor function. The compound is typically administered via intraperitoneal or oral routes at various doses depending on the experimental paradigm. Behavioral assays such as conditioned place preference, locomotor activity, and prepulse inhibition are used to evaluate the effects of D3 receptor blockade on reward, motor function, and sensorimotor gating. The compound's high selectivity allows for the specific interrogation of D3-mediated behaviors without confounding effects from D2 receptor blockade.
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| ADME/Pharmacokinetics |
FAUC-365 has a molecular weight of 462.44 and a molecular formula of C23H25Cl2N3OS. It is a solid at room temperature and is typically stored as a powder at -20°C for up to 3 years, with solution-based storage at -20°C for up to 6 months. Purity is >98%. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions and should be protected from light and moisture.
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| Toxicity/Toxicokinetics |
FAUC-365 is a research compound for laboratory use only and is not intended for human therapeutic applications. Standard laboratory safety precautions should be followed when handling the compound, as it may cause skin, eye, and respiratory irritation. The compound's high selectivity for D3 receptors over D2 receptors suggests a potentially favorable side effect profile compared to non-selective dopamine receptor antagonists, with a lower risk of extrapyramidal symptoms.
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| References | |
| Additional Infomation |
FAUC-365 (CAS 474432-66-1) is a novel, potent, and highly selective dopamine D3 receptor antagonist with a Ki of 0.5 nM. It demonstrates over 100-fold selectivity against D2 and D4 receptor subtypes. The compound is primarily utilized in research related to schizophrenia and Parkinson's disease. FAUC-365 serves as a valuable pharmacological tool for investigating D3 receptor function in neuropharmacology, with applications in both in vitro binding assays and in vivo models of addiction and neurological disorders.
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| Molecular Formula |
C23H25CL2N3OS
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|---|---|
| Molecular Weight |
462.43510222435
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| Exact Mass |
461.109
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| Elemental Analysis |
C, 59.74; H, 5.45; Cl, 15.33; N, 9.09; O, 3.46; S, 6.93
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| CAS # |
474432-66-1
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| PubChem CID |
10276451
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| Appearance |
Solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
680.3±55.0 °C at 760 mmHg
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| Flash Point |
365.2±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.638
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| LogP |
7.14
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
561
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C(=CC=CC=1N1CCN(CCCCNC(C2=CC3C=CC=CC=3S2)=O)CC1)Cl
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| InChi Key |
CPTSTFKVXWZGEV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25Cl2N3OS/c24-18-7-5-8-19(22(18)25)28-14-12-27(13-15-28)11-4-3-10-26-23(29)21-16-17-6-1-2-9-20(17)30-21/h1-2,5-9,16H,3-4,10-15H2,(H,26,29)
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| Chemical Name |
N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]-1-benzothiophene-2-carboxamide
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| Synonyms |
FAUC365; FAUC 365; FAUC-365
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| HS Tariff Code |
2934.99.03.00
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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: ~33.3 mg/mL (~72.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. 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 (5.41 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1624 mL | 10.8122 mL | 21.6244 mL | |
| 5 mM | 0.4325 mL | 2.1624 mL | 4.3249 mL | |
| 10 mM | 0.2162 mL | 1.0812 mL | 2.1624 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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