2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. LY2934747

LY2934747 是一种选择性和能透过血脑屏障的双重 mGlu2/mGlu3 受体激动剂，对人源受体的 Ki 值分别为 260 nM 和 177 nM，EC50 为 8.4 nM 和 62.4 nM。LY2934747 在体内动物模型中表现出抗精神病与镇痛活性。LY2934747 可用于精神病、疼痛相关研究。

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LY2934747

LY2934747 Chemical Structure

CAS No. : 1448707-43-4

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LY2934747 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LY2934747 is a selective and blood-brain barrier-permeable dual mGlu2/mGlu3 receptor agonist, with Ki values of 260 nM and 177 nM, and EC50 values of 8.4 nM and 62.4 nM against human receptors, respectively. LY2934747 exhibits antipsychotic and analgesic activities in in vivo animal models. LY2934747 can be used in studies related to psychosis and pain[1].

IC50 & Target[1]

mGlu2 Receptor

 

mGluR3R

 

体外研究
(In Vitro)

LY2934747 具有高水溶性和 DMSO 溶解性、低 MDCK 通透性、极低的肝脏代谢水平、无显著 Cyp 亚型抑制作用，且在多个物种中均具有高血浆游离分数[1]。

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

LY2934747 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-24 Cmax Tmax T1/2 Bioavailability C0 CL Vdss
Rat[1] 5 mg/kg i.v. 33661 nM·h / / 3.6 h / 76749 nM 11.8 mL/min/kg 0.57 L/kg
Rat[1] 5 mg/kg p.o. 2826 nM·h 530 nM 2 h 3.8 h 8 % / / /
Rat[1] 1 mg/kg i.p. 3050 nM·h 3580 nM 0.5 h 1.1 h 45 % / / /
Rat[1] 3 mg/kg i.p. 7310 nM·h 10300 nM 0.5 h 0.4 h 36 % / / /
Rat[1] 10 mg/kg i.p. 48500 nM·h 59000 nM 0.4 h 1.5 h 72 % / / /
体内研究
(In Vivo)

LY2934747 (0.3-10 mg/kg；腹腔注射；单剂量) 可剂量依赖性地减弱大鼠中 Phencyclidine (PCP) 诱导的高活动性[1]。
LY2934747 (0.3-10 mg/kg；腹腔注射；单剂量) 可呈剂量依赖性抑制大鼠 Formalin 诱导的伤害性反应，其 ED50 为 0.7 mg/kg[1]。
LY2934747 (0.3-10 mg/kg；腹腔注射；单剂量) 在 10 mg/kg 剂量下会诱导大鼠运动协调障碍，而在 3 mg/kg 剂量下未观察到该效应[1]。

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

Animal Model: Sprague-Dawley (male, 175-250 g)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose (4 hours prior to PCP challenge)
Result: Produced a dose-related reduction in horizontal ambulations.
Achieved statistically significant effects (p < 0.05) at 3 mg/kg and 10 mg/kg.
Reached a calculated ED50 of 1.5 mg/kg.
Animal Model: Sprague-Dawley (male, 200-240 g)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose (60 minutes prior to formalin injection)
Result: Produced a dose-related decrease in nociceptive responses in both the early (0-5 minutes) and late (11-40 minutes) phases.
Achieved statistically significant effects at 1 mg/kg, 3 mg/kg, and 10 mg/kg.
Reached a calculated ED50 of 0.7 mg/kg.
Animal Model: Sprague-Dawley (male)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose (1, 2, or 3 hours prior to testing)
Result: Produced statistically significant locomotor impairment at 10 mg/kg when tested 1, 2, and 3 hours post-administration.
Caused no impairment at the 3 mg/kg dose at any time point.
分子量

211.22

Formula

C10H13NO4
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

LY2934747 相关分类

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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:

LY29347471448707-43-4LY 2934747LY-2934747mGluRMetabotropic glutamate receptorsmGlu2 receptorspainmGlu receptor subtypesmGlu2 receptormGlu3 receptorCNS targetsrat cortical mGlu2/3 receptorsInhibitorinhibitorinhibit

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目录号：
HY-131288
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