| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
D3 Receptor ( EC50 = 1.5 nM )
FAUC-346 targets dopamine D3 receptor (D3R), with a Ki value of 0.8 nM (radioligand binding assay using [³H]-spiperone) [2] FAUC-346 shows high subtype selectivity for D3R over D2 receptor (D2R): Ki = 120 nM for D2R, resulting in a D2R/D3R selectivity ratio of 150 [2] |
|---|---|
| ln Vitro |
FAUC 346, an in vitro D3-selective ligand, has a Ki of 0.23 nM for D3 in CHO cells [1]. FAUC346 has certain affinity for 5HT1A receptor (Ki=41 nM) and α1 receptor (Ki=15 nM) [1].
D3R binding affinity: FAUC-346 (0.01–100 nM) dose-dependently displaced [³H]-spiperone binding to recombinant human D3R, achieving 95% displacement at 10 nM (radioligand binding assay) [2] - Dopamine receptor subtype selectivity: No significant binding to D1, D4, or D5 receptors at concentrations up to 1 μM (Ki > 1 μM for D1/D4/D5); D2R/D3R selectivity ratio of 150, confirming subtype-specific interaction with D3R [2] - High binding specificity: In membrane preparations from D3R-overexpressing cells, FAUC-346 exhibited specific binding fraction of 88% (non-specific binding defined by excess unlabeled spiperone) [2] |
| ln Vivo |
Brain penetration and D3R-specific uptake (mouse model): Intravenous administration of 18F-labeled FAUC-346 (10 MBq/mouse) resulted in rapid brain uptake, reaching peak concentration at 30 minutes post-injection (0.8% ID/g tissue) [2]
- Regional brain distribution: Highest uptake in D3R-rich brain regions (nucleus accumbens, ventral tegmental area) with uptake ratio (target/non-target region) of 3.2 (nucleus accumbens/cerebellum) at 60 minutes [2] - Specific binding confirmation: Co-administration of excess unlabeled FAUC-346 (1 mg/kg, iv) reduced 18F-labeled derivative uptake in D3R-rich regions by 75%, confirming D3R-specific binding in vivo [2] - Rapid clearance: Radioactivity cleared from non-target tissues with half-life of 45 minutes; <6% ID/g tissue remaining in brain at 2 hours post-injection [2] |
| Enzyme Assay |
Radioligand displacement assay for D3R: Recombinant human D3R-containing membrane preparations were incubated with [³H]-spiperone (0.5 nM) and serial dilutions of FAUC-346 (0.01–100 nM) in binding buffer at 25°C for 120 minutes. Bound and free radioligand were separated by filtration through glass fiber filters, and radioactivity was quantified to calculate Ki value [2]
- Subtype selectivity assay: Membrane preparations expressing human D2R, D1R, D4R, or D5R were used in the same radioligand displacement assay with FAUC-346 (0.01–1000 nM) to evaluate binding affinity for other dopamine receptor subtypes [2] |
| Animal Protocol |
In vivo PET imaging and biodistribution study: 6–8 weeks old CD-1 mice were anesthetized and injected intravenously with 18F-labeled FAUC-346 (10 MBq/mouse) via tail vein [2]
- Specific binding control: A separate group of mice received intravenous injection of unlabeled FAUC-346 (1 mg/kg) 15 minutes before administration of 18F-labeled derivative [2] - Sample collection and analysis: Mice were euthanized at 30, 60, and 120 minutes post-injection. Brain regions (nucleus accumbens, ventral tegmental area, cerebellum) and peripheral tissues (liver, kidney, blood) were dissected, weighed, and radioactivity was measured to calculate percent injected dose per gram tissue (% ID/g) [2] - Drug formulation: Unlabeled FAUC-346 was dissolved in dimethyl sulfoxide (DMSO) and diluted with physiological saline (final DMSO concentration ≤5%) for intravenous injection; 18F-labeled derivative was formulated in saline containing 10% ethanol [2] |
| ADME/Pharmacokinetics |
Brain penetration: 30 minutes after injection, the uptake of 18F-labeled FAUC-346 in the brain reached its peak (0.8% ID/g) [2]
- Regional distribution in the brain: The uptake in areas rich in D3 receptors (nucleus accumbens, ventral tegmental area) was 3.0-3.2 times higher than in the cerebellum (D3 receptor-poor area) [2] - Clearance: The half-life of the radioactive material in the brain was 55 minutes; the brain clearance rate exceeded 70% within 2 hours after injection [2] - Peripheral clearance: Rapid clearance from the blood (t₁/₂ = 30 minutes); mainly excreted by the kidneys (35% ID in urine 2 hours later) [2] |
| References |
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| Additional Infomation |
FAUC-346 is a synthetic small molecule ligand with high subtype selectivity for dopamine D3 receptor (D3R)[2] - It can serve as a lead compound for the development of 18F-labeled PET radioligands for non-invasive imaging of D3R in the central nervous system (CNS)[2] - Its mechanism of action involves high affinity binding to the orthotopic site of D3R with very low cross-reactivity with other dopamine receptor subtypes, especially D2R[2] - Potential applications include PET diagnosis of neuropsychiatric disorders associated with D3R dysregulation (e.g., schizophrenia, addiction, Parkinson's disease)[2] - The compound's good brain penetration, rapid clearance, and high D3R specificity make it an ideal framework for PET imaging probes targeting the CNS[2]
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| Molecular Formula |
C24H29N3O2S
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|---|---|
| Molecular Weight |
423.570964574814
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| Exact Mass |
423.198
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| CAS # |
474432-65-0
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| PubChem CID |
9888555
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| Appearance |
White to off-white solid powder
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| LogP |
4.9
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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 |
30
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| Complexity |
541
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KFMBPIZMZUDONQ-UHFFFAOYSA-
|
| InChi Code |
InChI=1S/C24H29N3O2S/c1-29-21-10-4-3-9-20(21)27-16-14-26(15-17-27)13-7-6-12-25-24(28)23-18-19-8-2-5-11-22(19)30-23/h2-5,8-11,18H,6-7,12-17H2,1H3,(H,25,28)
|
| Chemical Name |
N-[4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl]-1-benzothiophene-2-carboxamide
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| Synonyms |
FAUC346; FAUC 346; FAUC-346
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~236.1 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.90 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 (5.90 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 | 2.3609 mL | 11.8044 mL | 23.6088 mL | |
| 5 mM | 0.4722 mL | 2.3609 mL | 4.7218 mL | |
| 10 mM | 0.2361 mL | 1.1804 mL | 2.3609 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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