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Carabersat

Catalog No. T14863 CAS 184653-84-7

Synonyms: SB 204269

Carabersat（SB 204269） is a novel and effective anticonvulsant and antiepileptic agent.

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Carabersat, CAS 184653-84-7

Pack Size	Availability	Price/USD	Quantity
1 mg	In stock	$ 700.00
5 mg	In stock	$ 1,800.00

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Purity: 100%

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Description	Carabersat（SB 204269） is a novel and effective anticonvulsant and antiepileptic agent.
Targets&IC50	Forebrain membranes:53 nM (Kd,mouse), Forebrain membranes:40 nM (Kd,rat), Forebrain membranes:7.3 (pKi,rat)
In vitro	[3H]Carabersat ([3H]SB 204269) binds to rat forebrain membranes with moderate affinity (Kd 40 nM) and pKi values of 7.3[1]. In mouse forebrain membranes, Carabersat is able to bind, and the binding is saturable and stereospecific, with a Kd of 53 nM. The labeled [3H]Carabersat produces a Kd of 32 nM[2]. Carabersat (SB-204269, 1-100 μM) has no effect on Na+ current in cultured hippocampal neurons. It also shows no effect on action potential discharges evoked by elevating external K+[4]. Structurally related to the benzopyran ATP-sensitive potassium channel (KATP) opener cromakalim, Carabersat (SB-204269) has opposite stereochemistry, and its mechanism of action is not thought to involve KATP[3].
In vivo	Significantly elevating anticonvulsant activity in mice, Carabersat (5b) has been observed[1].

Synonyms	SB 204269
Molecular Weight	357.38
Formula	C20H20FNO4
CAS No.	184653-84-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Wai N. Chan, et al. Synthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile. J. Med. Chem., 1996, 39 (23), pp 4537-4539. 2. Herdon H, et al. The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain. Eur J Pharmacol. 1996 Oct 31;314(3):R7-8. 3. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8. 4. Caeser M, et al. Lack of effect of the novel anticonvulsant SB-204269 on voltage-dependent currents in neurones cultured from rat hippocampus. Neurosci Lett. 1999 Aug 13;271(1):57-60.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Carabersat 184653-84-7 Others SB 204269 inhibitor inhibit

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