2. GPCR/G Protein
  3. Trace Amine-associated Receptor (TAAR)
  4. LK00764

LK00764 是一种 TAAR1 激动剂，EC50 为 4 nM。LK00764 可缓解 Dizocilpine (HY-15084B) 诱导的运动过度活跃，降低垂直运动活性，减轻多巴胺转运体敲除大鼠的自发性运动过度活跃，并抑制大鼠的应激诱导性体温过高。LK00764 可用于精神分裂症的研究。

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LK00764

LK00764 Chemical Structure

CAS No. : 2916446-33-6

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LK00764 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

LK00764 可在瞬时转染的 HEK-293 细胞中强效激活 TAAR1，其 EC50 为 4.0 nM[1]。
LK00764 可通过亲脂相互作用、π-π 堆积作用、盐桥和氢键相互作用网络，以高亲和力与 TAAR1 稳定结合[1]。

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

LK00764 相关抗体:
体内研究
(In Vivo)

LK00764 (0.3-10 mg/kg; 腹腔注射; 单次) 在大鼠中展现 TAAR1 激动活性，并在 MK‑801 (HY-15084B) 诱导多动、DAT 敲除大鼠多动及应激性高热模型中呈现抗精神病与抗焦虑样效果[1]。

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.
分子量

298.77

Formula

C16H15ClN4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

LK00764 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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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