1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Flindokalner

Flindokalner (Synonyms: BMS-204352)

Cat. No.: HY-108584
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Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.

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Flindokalner Chemical Structure

Flindokalner Chemical Structure

CAS No. : 187523-35-9

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10 mM * 1 mL in DMSO USD 475 In-stock
Estimated Time of Arrival: December 31
5 mg USD 600 In-stock
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Description

Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo[1][2].

IC50 & Target

Ki: 3.7 μM (Kv7.1), 230 μM (Kv7.4), 605 μM (Kv7.5)[1]

In Vitro

Flindokalner (BMS-204352) (10 μM) inhibits Kv7.4and Kv7.5 with Kis of 230 and 605 μM, respectively[1].
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[2].

In Vivo

Flindokalner (BMS-204352) (3-30 mg/kg; i.p.) induces a dose-dependent anxiolytic effect[1].
In shock-based conditioned model of anxiety in male Wistar rats, Flindokalner (3-60 mg/kg; i.p.) engenderes an anxiolytic profile[1].

Animal Model: Female NMRI or male C57 mice (20-25 g) (Anxiolytic Models)[1]
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.
Molecular Weight

359.70

Formula

C₁₆H₁₀ClF₄NO₂

CAS No.

187523-35-9

SMILES

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

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

FlindokalnerBMS-204352BMS204352BMS 204352Potassium ChannelKcsAneuronalsubtypeanxiolyticcurrentventricularmyocyteseffectsInhibitorinhibitorinhibit

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