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Flindokalner

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Chemical Structure| 187523-35-9 同义名 : BMS-204352;(+)-BMS 204352;MaxiPost.
CAS号 : 187523-35-9
货号 : A854541
分子式 : C16H10ClF4NO2
纯度 : 98%
分子量 : 359.703
MDL号 : MFCD09475617
存储条件:

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(291.91 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Flindokalner ,also known as BMS-204352, is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel isoforms expressed in HEK293 cells. Flindokalner is also a BKca-positive modulator. Flindokalner has a negative regulatory activity (Ki=3.0) on Kv7.1 channels. Flindokalner has negative modulatory activity on Kv7.1 channels (Ki=3.7 μM) and acts as a negative modulator of GABAA receptors. Flindokalner has anxiolytic efficacy in vivo[1][2].At a concentration of 10 μM, Flindokalner inhibits Kv7.4 and Kv7.5 with Ki values of 230 μM and 605 μM, respectively[1].In the concentration range of 1-10 μM, Flindokalner inhibited Ca2+ currents in a dose-dependent manner with a Kd value of 6 μM and a Hill coefficient of 1.33. In freshly isolated rat ventricular myocytes, Flindokalner inhibited cardiac L-type Ca2+ channels in a direct manner without affecting BKCa channels or intracellular signaling[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.90mL

2.78mL

1.39mL

27.80mL

5.56mL

2.78mL

参考文献

[1]Korsgaard MP, et al. Anxiolytic effects of Maxipost (BMS-204352) and retigabine via activation of neuronal Kv7channels. J Pharmacol Exp Ther. 2005 Jul;314(1):282-92.

[2]Son YK, et al. The inhibitory effect of Ca2+-activated K+ channel activator, BMS on L-type Ca2+ channels in rat ventricular myocytes. Life Sci. 2011 Aug 29;89(9-10):331-6.