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MedChemExpressModel Tonabersat -175013-84-0

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Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system[1][2][3].
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Tonabersat

MCE China:Tonabersat

Brand:MedChemExpress (MCE)

Cat. No.HY-15204

CAS:175013-84-0

Synonyms:SB-220453

Purity:98.36%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system.

In Vitro:Tonabersat, a novel benzopyran derivative, inhibits cortical spreading depression (CSD) and therefore might be able to inhibit the early migraine mechanisms[1].

In Vivo:Tonabersat (10 mg/kg) significantly inhibits progression of metastatic lesions. Addition of NSC 241240 to either agent profoundly inhibits brain metastasis[2].

Animal Administration:Mice[2] Athymic NCR nu/nu mice, Cr:NIH bg-nu-xid mice, B6129SF1/J, C57BL/6J-Tmem173gt/J 'golden ticket', and C57/Bl/6J mice are used at 5-6 weeks of age. For inducible knockdown experiments, mice are given WC2031 in the drinking water (2 mg/mL) and the diet 14 days after injection of cancer cells. For drug treatment experiments, mice are intraperitoneally injected with NSC 241240 (5 mg/kg per 5 days), Tonabersat (MedChem Express) (10 mg/kg per day), or meclofenamic acid sodium salt (20 mg/kg per day). Vehicle (10% DMSO in polyethylene glycol 400) is used in control mice. Quantification of tumour burden is by Bio-luminescent imaging (BLI), performed using an IVIS Spectrum Xenogen instrument and analysed using Living Image software v.2.50.

IC50 & Target:Gap-junction[1] In Vitro Tonabersat, a novel benzopyran derivative, inhibits cortical spreading depression (CSD) and therefore might be able to inhibit the early migraine mechanisms[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Tonabersat Related Antibodies

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References:

[1]. Silberstein SD, et al. Tonabersat, a gap-junction modulator: efficacy and safety in two randomized, placebo-controlled, dose-ranging studies of acute migraine. Cephalalgia. 2009 Nov;29 Suppl 2:17-27.  [Content Brief]

[2]. Chen Q, et al. Carcinoma-astrocyte gap junctions promote brain metastasis by cGAMP transfer. Nature. 2016 May 18;533(7604):493-8.  [Content Brief]

[3]. Kim Y, et al. Tonabersat Prevents Inflammatory Damage in the Central Nervous System by Blocking Connexin43 Hemichannels. Neurotherapeutics. 2017 May 30.  [Content Brief]

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