Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μM for mGlu5a, LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis.
ターゲット&IC50 | mGluR1a:8.8 μM |
In vivo | LY367385 effectively suppresses sound-induced clonic seizures in DBA/2 mice with a rapid onset, achieving a median effective dose (ED50) of 12 nM when administered intracerebroventricularly (i.c.v.) 5 minutes prior. It also significantly reduces the frequency of spontaneous electroencephalogram (EEG) spike and wave discharges in lethargic (lh/lh) mice, maintaining this effect from 30 to over 150 minutes post-administration at a concentration of 250 nM, i.c.v. Furthermore, LY367385 has been utilized in both DBA/2 and lethargic mice, in addition to direct application into the inferior colliculus of genetically epilepsy-prone rats (GEPR), demonstrating its efficacy in reducing seizures across different models. Specifically, in GEPR, a bilateral dose of 160 nM substantially mitigates clonic seizures within 2-4 hours. |
分子量 | 209.2 |
分子式 | C10H11NO4 |
CAS No. | 198419-91-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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LY367385 198419-91-9 Metabolism FXR LY-367385 LY 367385 Inhibitor inhibitor inhibit