2. GPCR/G Protein
  3. Trace Amine-associated Receptor (TAAR)
  4. 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.

LK00764

LK00764 Chemical Structure

CAS No. : 2916446-33-6

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LK00764 Related Antibodies

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Description

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[1].

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.

LK00764 Related Antibodies
In Vivo

LK00764 (0.3-10 mg/kg; i.p.; single administration) exhibits TAAR1 agonist activity in rats, and shows antipsychotic and anxiolytic-like effects in MK‑801 (HY-15084B)-induced hyperactivity, DAT knockout rat hyperactivity, and stress-induced hyperthermia models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats (3-4 months old, male, MK-801-induced hyperactivity model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.p.; single dose
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.
Animal Model: Dopamine transporter knockout (DAT-KO) rats (spontaneous locomotor hyperactivity model)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose
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.
Animal Model: Wistar rats (male, stress-induced hyperthermia model)[1]
Dosage: 3 mg/kg; 5 mg/kg
Administration: i.p.; single dose
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.
Molecular Weight

298.77

Formula

C16H15ClN4
CAS No.
SMILES

ClC1=CC=C(C2=CC=C(C3=NN=C(CCN)N3)C=C2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LK00764 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LK007642916446-33-6LK 00764LK-00764Trace Amine-associated Receptor (TAAR)schizophreniaMK-801-induced locomotor hyperactivityβ-phenylethylamineDAT-KO ratsTAAR1dopamine transporter knockout ratsstress-induced hyperthermiaHEK-293 cellsWistar ratsTrace Amine-Associated Receptor 1Inhibitorinhibitorinhibit

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