LY456236|cas:338736-46-2|西域试剂

LY456236,99.81%

产品编号：Bellancom-103566| CAS NO：338736-46-2| 分子式：C₁₆H₁₆ClN₃O₂| 分子量：317.77

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-103566		￥4580.00	杭州北京（现货）

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LY456236

产品介绍

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。

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.

体外研究

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

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

Cell Proliferation Assay

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。

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

Animal Model:	DBA/2 mice and CD1 mice, seizure models
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
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.

体内研究

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。

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

Animal Model:	DBA/2 mice and CD1 mice, seizure models
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
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.

体内研究

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。

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

Animal Model:	DBA/2 mice and CD1 mice, seizure models
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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (786.73 mM; ultrasonic and warming and heat to 60°C)

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
10 mM	0.3147 mL	1.5735 mL	3.1469 mL

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。

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)

参考文献