2. GPCR/G Protein Neuronal Signaling JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. mGluR EGFR
  4. LY456236

LY456236 是一种选择性、非竞争性和具有口服活性的 mGlu1 受体拮抗剂，可抑制磷酸肌醇水解，其 IC50 为 0.145 μM。LY456236 还能抑制 EGFR，IC50 为 0.91 μM。

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LY456236 Chemical Structure

LY456236 Chemical Structure

CAS No. : 338736-46-2

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5 mg ￥2862
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10 mg ￥4000
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Customer Review

LY456236 相关抗体

Top Publications Citing Use of Products

查看 mGluR 亚型特异性产品:

查看所有亚型
mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM[1][3].

IC50 & Target

IC50: 0.145 μM (mGlu1), 0.91 μM (EGFR)[1]
体外研究
(In Vitro)

LY456236 (2 μM; 30 min) 降低 DHPG (HY-12598A) 刺激的 OCCM-30 增殖[2]。

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

LY456236 相关抗体:

Cell Proliferation Assay[2]

Cell Line: OCCM-30 cells
Concentration: 2 μM
Incubation Time: 30 min, followed by 72 h incubation with DHPG (HY-12598A)
Result: Reduced DHPG-stimulated OCCM-30 proliferation.
体内研究
(In Vivo)

LY456236 在小鼠 (3-100 mg/kg; i.p.; once) 和大鼠 (10-60 mg/kg; oral; once) 中显示抗惊厥作用。

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

Animal Model: DBA/2 mice and CD1 mice, seizure models[3]
Dosage: 3-100 mg/kg
Administration: IP, once
Result: Produced dose-related anticonvulsant effects in preventing audiogenic-induced (tonic-clonic) seizures in DBA/2 mice, threshold electroshock-induced seizures in CD1 mice, and 6 Hz electroshock-induced seizures in CD1 mice.
Animal Model: Amygdala-kindled Sprague-Dawley rats[3]
Dosage: 10, 30 and 60 mg/kg
Administration: Oral, once
Result: Produced dose-related decreases in behavioral and electrographic seizures at threshold stimulus intensity. Produced a dose-related increase in the stimulus intensity required to produce generalized seizures.
分子量

317.77

Formula

C16H16ClN3O2
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 250 mg/mL (786.73 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1469 mL 15.7347 mL 31.4693 mL
5 mM 0.6294 mL 3.1469 mL 6.2939 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

LY456236 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1469 mL 15.7347 mL 31.4693 mL 78.6733 mL
5 mM 0.6294 mL 3.1469 mL 6.2939 mL 15.7347 mL
10 mM 0.3147 mL 1.5735 mL 3.1469 mL 7.8673 mL
15 mM 0.2098 mL 1.0490 mL 2.0980 mL 5.2449 mL
20 mM 0.1573 mL 0.7867 mL 1.5735 mL 3.9337 mL
25 mM 0.1259 mL 0.6294 mL 1.2588 mL 3.1469 mL
30 mM 0.1049 mL 0.5245 mL 1.0490 mL 2.6224 mL
40 mM 0.0787 mL 0.3934 mL 0.7867 mL 1.9668 mL
50 mM 0.0629 mL 0.3147 mL 0.6294 mL 1.5735 mL
60 mM 0.0524 mL 0.2622 mL 0.5245 mL 1.3112 mL
80 mM 0.0393 mL 0.1967 mL 0.3934 mL 0.9834 mL
100 mM 0.0315 mL 0.1573 mL 0.3147 mL 0.7867 mL
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:

LY456236338736-46-2LY 456236LY-456236mGluREGFRMetabotropic glutamate receptorsEpidermal growth factor receptorErbB-1HER1anticonvulsantDHPGOCCM-30DBA/2CD1 miceseizureInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-103566
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