DAT-IN-2
DAT-IN-2 is an atypical dopamine transporter (DAT) inhibitor with blood-brain barrier permeability. DAT-IN-2 binds to human DAT with a Ki of 63.0 nM and stabilizes the transporter in an inward-facing conformation. DAT-IN-2 produces only weak locomotor stimulant effects and does not induce conditioned place preference in mice, indicating no rewarding effects. DAT-IN-2 can be used in research related to psychostimulant use disorder.
For research use only. We do not sell to patients.
- Formula: C17H12Cl2FNOS2
- Molecular Weight:400.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
DAT-IN-2 (compound 32b) binds with high affinity and selectivity to hDAT in HEK293 cell membranes[1].
DAT-IN-2 is an atypical dopamine transporter (DAT) inhibitor with a Ki of 63.0 nM for hDAT[1].
DAT-IN-2 is metabolically stable in mouse and rat liver microsomes, with half-lives of 16 min and 26 min, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Tmax |
|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 0.5 h |
In Vivo
DAT-IN-2 (10-30 mg/kg; i.p.) effectively penetrates brain tissue and significantly enhances DA-dependent brain stimulation reward at a dose of 30 mg/kg; it does not produce rewarding effects in the conditioned place preference model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Webster (male, 30-40 g)[1]
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Dosage:3, 10, 30 mg/kg
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Administration:i.p.
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Result:Produced only modest increase in ambulatory distance exclusively at the highest 30 mg/kg dose compared with vehicle group.
No obvious body‑weight loss or mortality was observed in tested animals.
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Animal Model:Swiss Webster mice (male, 30‑40 g)[1]
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Dosage:10, 30 mg/kg
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Administration:Intraperitoneal (IP) injection; alternate days during the 10-day conditioning phase within a total 14-day CPP schedule (2 days preconditioning, 10 days conditioning, 2 days CPP testing)
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Result:Showed no significant conditioned place preference response compared with vehicle group.
Did not induce rewarding or aversive behavioral phenotypes at tested doses.
Chemical Information
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Molecular Weight 400.32
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Formula C17H12Cl2FNOS2
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SMILES
FC1=CC(C2=CC=C(Cl)C(Cl)=C2)=C(C[S@@](CC3=CN=CS3)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DAT-IN-2 Related Classifications
HY-189362 Related Classifications
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Keywords
- DAT-IN-2
- Dopamine Transporter
- blood-brain barrier crossing
- hERG channel activity
- inward-facing conformation
- dopamine-dependent optical brain-stimulation reward
- psychostimulant use disorder
- mouse and rat liver microsomes
- brain-to-blood ratios
- HEK293 cell membranes
- human DAT
- atypical dopamine transporter (DAT) inhibitor
- Inhibitor
- inhibitor
- inhibit