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  • Product Name: BMS-204352
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

187523-35-9

187523-35-9 structure
187523-35-9 structure
  • Name: MaxiPost
  • Chemical Name: (3S)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1H-indol-2-one
  • CAS Number: 187523-35-9
  • Molecular Formula: C16H10ClF4NO2
  • Molecular Weight: 359.70300
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
  • Create Date: 2016-12-06 03:39:00
  • Modify Date: 2024-01-10 18:10:13
  • 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].

Name (3S)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1H-indol-2-one
Synonyms [14C]-Flindokalner
MaxiPost
(3S)-3-(5-Chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1,3-dihydro-2H-indol-2-one
(3S)-(+)-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indol-2-one
(S)-(+)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-trifluoromethyl-1,3-dihydroindol-2-one
Flindokalner
Flindokalner [USAN:INN]
Maxipost (TN)
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].
Related Catalog
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.
References

[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.

Density 1.5g/cm3
Boiling Point 436.9ºC at 760mmHg
Molecular Formula C16H10ClF4NO2
Molecular Weight 359.70300
Flash Point 218ºC
Exact Mass 359.03400
PSA 38.33000
LogP 4.67060
Vapour Pressure 7.82E-08mmHg at 25°C
Index of Refraction 1.574
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P280-P304 + P340 + P312-P305 + P351 + P338-P337 + P313
RIDADR NONH for all modes of transport
RTECS NM3249000

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187523-35-9 structure

187523-35-9

Literature: Bristol-Myers Squibb Company Patent: EP946173 B1, 2005 ; Location in patent: Page/Page column 12 ;

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187523-35-9

Literature: Li, Jun; Cai, Yunfei; Chen, Weiliang; Liu, Xiaohua; Lin, Lili; Feng, Xiaoming Journal of Organic Chemistry, 2012 , vol. 77, # 20 p. 9148 - 9155,8 Title/Abstract Full Text Show Details Li, Jun; Cai, Yunfei; Chen, Weiliang; Liu, Xiaohua; Lin, Lili; Feng, Xiaoming Journal of Organic Chemistry, 2012 , vol. 77, # 20 p. 9148 - 9155

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187523-35-9 structure

187523-35-9

Literature: Hamashima, Yoshitaka; Suzuki, Toshiaki; Takano, Hisashi; Shimura, Yuta; Sodeoka, Mikiko Journal of the American Chemical Society, 2005 , vol. 127, # 29 p. 10164 - 10165

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187523-35-9 structure

187523-35-9

Literature: Hamashima, Yoshitaka; Suzuki, Toshiaki; Takano, Hisashi; Shimura, Yuta; Sodeoka, Mikiko Journal of the American Chemical Society, 2005 , vol. 127, # 29 p. 10164 - 10165

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187523-35-9 structure

187523-35-9

Literature: Hamashima, Yoshitaka; Suzuki, Toshiaki; Takano, Hisashi; Shimura, Yuta; Sodeoka, Mikiko Journal of the American Chemical Society, 2005 , vol. 127, # 29 p. 10164 - 10165

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187523-35-9 structure

187523-35-9

Literature: Hamashima, Yoshitaka; Suzuki, Toshiaki; Takano, Hisashi; Shimura, Yuta; Sodeoka, Mikiko Journal of the American Chemical Society, 2005 , vol. 127, # 29 p. 10164 - 10165

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187523-35-9 structure

187523-35-9

Literature: Zoute, Ludivine; Audouard, Christophe; Plaquevent, Jean-Christophe; Cahard, Dominique Organic and biomolecular chemistry, 2003 , vol. 1, # 11 p. 1833 - 1834

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187523-35-9 structure

187523-35-9

Literature: Zoute, Ludivine; Audouard, Christophe; Plaquevent, Jean-Christophe; Cahard, Dominique Organic and biomolecular chemistry, 2003 , vol. 1, # 11 p. 1833 - 1834

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187523-35-9 structure

187523-35-9

Literature: Hewawasam, Piyasena; Gribkoff, Valentin K.; Pendri, Yadagiri; Dworetzky, Steven I.; Meanwell, Nicholas A.; Martinez, Eduardo; Boissard, Christopher G.; Post-Munson, Debra J.; Trojnacki, Joanne T.; Yeleswaram, Krishnaswamy; Pajor, Lorraine M.; Knipe, Jay; Gao, Qi; Perrone, Robert; Starrett Jr., John E. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 7 p. 1023 - 1026