LY 456236 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.

Animal Model:DBA/2 mice and CD1 mice, seizure modelsDosage:3-100 mg/kgAdministration:IP, onceResult: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.

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Angiogenesis

EGFR

EGFR | GluR

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338736-46-2

317.77

C16H16ClN3O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (786.73 mM; 超声助溶 (<60°C)

Cl.COc1ccc(Nc2ncnc3ccc(OC)cc23)cc1

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(-20℃)

With Ice Pack

≥ 2 years