LK00764
LK00764 is a TAAR1 agonist with an EC50 of 4 nM. LK00764 alleviates Dizocilpine (HY-15084B)-induced hyperlocomotion, reduces vertical locomotor activity, attenuates spontaneous hyperlocomotion in dopamine transporter knockout rats, and inhibits stress-induced hyperthermia in rats. LK00764 can be used for the research of schizophrenia.
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- CAS No.: 2916446-33-6
- Formule: C16H15ClN4
- Masse moléculaire:298.77
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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TAAR1 |
LK00764 potently activates TAAR1 in transiently transfected HEK-293 cells, with an EC50 of 4.0 nM[1].
LK00764 binds stably to TAAR1 with high affinity via a network of lipophilic interactions, π-π stacking interactions, salt bridges and hydrogen bonds[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (3-4 months old, male, MK-801-induced hyperactivity model)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Dose-dependently mitigated MK-801-induced hyperactivity.
Produced a significant reduction in both horizontal and vertical locomotor activity at 5 mg/kg and 10 mg/kg compared to vehicle control.
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Animal Model:Dopamine transporter knockout (DAT-KO) rats (spontaneous locomotor hyperactivity model)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Produced a dose-dependent decrease in both horizontal and vertical locomotor hyperactivity.
Produced a significant reduction in both horizontal and vertical activity at 10 mg/kg compared to vehicle control.
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Animal Model:Wistar rats (male, stress-induced hyperthermia model)[1]
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Dosage:3 mg/kg; 5 mg/kg
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Administration:i.p.; single dose
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Result:Suppressed stress-induced hyperthermia at both tested doses.
Produced a significant reduction at 3 mg/kg and a highly significant reduction at 5 mg/kg compared to vehicle control.
Chemical Information
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CAS No. 2916446-33-6
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Masse moléculaire 298.77
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Formule C16H15ClN4
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SMILES
ClC1=CC=C(C2=CC=C(C3=NN=C(CCN)N3)C=C2)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)
LK00764 Related Classifications
HY-183428 Related Classifications
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- LK00764
- 2916446-33-6
- LK 00764
- LK-00764
- Trace Amine-associated Receptor (TAAR)
- schizophrenia
- MK-801-induced locomotor hyperactivity
- β-phenylethylamine
- DAT-KO rats
- TAAR1
- dopamine transporter knockout rats
- stress-induced hyperthermia
- HEK-293 cells
- Wistar rats
- Trace Amine-Associated Receptor 1
- Inhibitor
- inhibitor
- inhibit