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Art. -Nr.: HY-183428

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2916446-33-6
Formel: C₁₆H₁₅ClN₄
Molecular Weight:298.77

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

LK00764 Chemical Structure

CAS. Nr.: 2916446-33-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 2916446-33-6
Molecular Weight 298.77
Formel C₁₆H₁₅ClN₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Krasavin M, et al. Discovery of Trace Amine-Associated Receptor 1 (TAAR1) Agonist 2-(5-(4′-Chloro-[1, 1′-biphenyl]-4-yl)-4 H-1, 2, 4-triazol-3-yl) ethan-1-amine (LK00764) for the Treatment of Psychotic Disorders. Biomolecules. 2022 Nov 7;12(11):1650.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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