FAUC-365 |
Catalog No.GC12466
One-Click Copy Product Info
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D3 dopamine receptor agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 474432-66-1
Sample solution is provided at 25 µL, 10mM.
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FAUC-365 is a D3 dopamine receptor agonist.
The dopamine D3 receptor, first identified in 1990, is preferentially expressed in the nucleus accumbens, where dopamine is released by neurons originating from the ventral tegmental area. Convincing pharmacological studies implicate D3-mediated neurotransmission in the reinforcing effects of cocaine. It is therefore a target for drugs which treat drug addiction, schizophrenia, as well as Parkinson's disease.
In vitro: FAUC-365 was discovered by a rational and interactive SAR sequence. As a dichloro derivative, FAUC-365 revealed D3 affinities that were comparable to its methoxy-substituted analogues, however, the selectivities of FAUC-365 against 5HT-1A, 5-HT2, and R1 were substantially higher, which was demonstrated by that extraordinary selectivity ratios of 17600, 7200, 5200, and 680 over D1, D2long, D2short, and D4, respectively, were determined for FAUC-365 with Ki of 0.50 nM. In addition, the benzothiophene analog FAUC 346 and its oxa analogue showed partial agonist character with EC50 values at 0.36 and 1.5 nM, respectively [1].
In vivo: Up to now, there is no animal in vivo data reported for FAUC-365.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Bettinetti L, Schlotter K, Hübner H, Gmeiner P. Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. J Med Chem. 2002 Oct 10;45(21):4594-7.
| Cas No. | 474432-66-1 | SDF | |
| Chemical Name | N-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]-benzo[b]thiophene-2-carboxamide | ||
| Canonical SMILES | ClC1=C(Cl)C(N2CCN(CCCCNC(C3=CC4=C(C=CC=C4)S3)=O)CC2)=CC=C1 | ||
| Formula | C23H25CI2N3OS | M.Wt | 462.4 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.25 mg/ml,Ethanol: 2 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1626 mL | 10.8131 mL | 21.6263 mL |
| 5 mM | 432.5 μL | 2.1626 mL | 4.3253 mL |
| 10 mM | 216.3 μL | 1.0813 mL | 2.1626 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)