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.
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- Formule: C17H12Cl2FNOS2
- Masse moléculaire:400.32
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
In Vitro
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.
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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Masse moléculaire 400.32
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
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