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Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
5 mg | $77 | In Stock | |
10 mg | $113 | In Stock | |
25 mg | $238 | In Stock | |
50 mg | $355 | In Stock | |
100 mg | $507 | In Stock | |
1 mL x 10 mM (in DMSO) | $86 | In Stock |
Description | Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo. |
Targets&IC50 | Kv7.5:605 μM(Ki), Kv7.4:230 μM(Ki), Kv7.1:3.7 μM(Ki) |
In vitro | Flindokalner inhibits cardiac L-type Ca2+ channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes. Flindokalner (10 μM) inhibits Kv7.4and Kv7.5 (Kis: 230 and 605 μM, respectively)[1]. Flindokalner (1-10 μM) causes inhibition of the Ca2+ current in a dose-dependent manner (Kd: 6 μM and a Hill coefficient: 1.33) [2]. |
In vivo | Flindokalner (3-60 mg/kg; i.p.) engenders an anxiolytic profile, in a shock-based conditioned model of anxiety in male Wistar rats. Flindokalner (3-30 mg/kg; i.p.) induces a dose-dependent anxiolytic effect [1]. |
Alias | BMS-204352 |
Molecular Weight | 359.7 |
Formula | C16H10ClF4NO2 |
Cas No. | 187523-35-9 |
Smiles | COc1ccc(Cl)cc1[C@]1(F)C(=O)Nc2cc(ccc12)C(F)(F)F |
Relative Density. | 1.50 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (278.01 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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