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.
For research use only. We do not sell to patients.
- CAS No.: 2916446-33-6
- Formula: C16H15ClN4
- Molecular Weight:298.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
TAAR1 |
In Vitro
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. Further protocols information, click here.
In Vivo
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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Molecular Weight 298.77
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Formula 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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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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Gene Editing
Gene editing modify specific sites within the genome through gene deletions, insertions or conversions to study functionally unknown genes or conduct gene therapy. It is also used to change the biological traits of organisms to establish new varieties. Gene editing techniques include zinc finger nuclease (ZFN), transcription activator-like effector nuclease (TALEN), and clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR-associated protein 9 (Cas 9) (CRISPR/Cas9).
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Protocol for Open Field Test (OF)
The Open Field Test is a rodent behavioral assay that measures spontaneous locomotion, exploratory behavior, and anxiety-like behavior when an animal is placed in a novel open arena. The main readouts are total distance traveled, movement time, velocity, center-zone entries, center-zone time, peripheral-zone time, and thigmotaxis. The assay is based on the conflict between exploration of a novel environment and avoidance of exposed open areas; higher center exploration is commonly interpreted as lower anxiety-like behavior, whereas increased wall-following or peripheral occupancy is interpreted as higher anxiety-like behavior.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- 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