BMS-204352

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

一种强效且有效的 maxi-K 钾通道 (maxi-K) 钙敏感开放剂，在 HEK293 分离的外侧膜贴片中，EC50 为 392 nM（-48.4 mV）。

A potent and effective calcium-sensitive opener of maxi-K potassium channels (maxi-K) with EC50 of 392 nM at -48.4 mV in HEK293 isolated outside-out membrane patches; a potent and effective opener of two important subtypes of neuronal potassium channels, K(Ca) channels and KCNQ channels, strongly activates the voltage-gated K+ channel KCNQ5 with EC50 of 2.4 uM; shows significant levels of cortical neuroprotection in rat models of permanent large-vessel stroke.Stroke Phase 3 Discontinued.

Flindokalner (BMS-204352) (10 μM) inhibits Kv7.4and Kv7.5 with Kis of 230 and 605 μM, respectively.Flindokalner (1-10 μM) causes inhibition of the Ca2+ current in a dose-dependent manner, with a Kd of 6 μM and a Hill coefficient of 1.33. Flindokalnerinhibits cardiac L-type Ca2+ channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes.

Flindokalner (BMS-204352) (3-30 mg/kg; i.p.) induces a dose-dependent anxiolytic effect.In shock-based conditioned model of anxiety in male Wistar rats, Flindokalner (3-60 mg/kg; i.p.) engenderes an anxiolytic profile. Animal Model:Female NMRI or male C57 mice (20-25 g) (Anxiolytic Models)Dosage:i.p.Administration:3, 10, 30 mg/kg Result:Significantly and dose dependently increased time spent in the open areas, reduced latency to enter an open area, and increased the number of entries in to the open areas in Zero Maze.

BMS 204352 | Maxipost | BMS204352

Cell Cycle/DNA Damage

Potassium Channel

Potassium Channel

Neurological Disease

Stroke

187523-35-9

359.7

C16H10ClF4NO2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (278.01 mM)

O=C1NC2=C(C=CC(C(F)(F)F)=C2)[C@@]1(C3=CC(Cl)=CC=C3OC)F

(3S)-(+)-(5-Chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indole-2-one

(-20℃)

With Ice Pack

≥ 2 years