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[CAS NO. 175013-84-0] Tonabersat
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15204 |
| Brand: | MCE |
| CAS: | 175013-84-0 |
Overview
| MDL | MFCD00944458 |
|---|---|
| Molecular Weight | 391.82 |
| Molecular Formula | C20H19ClFNO4 |
| SMILES | O[C@@H]1C(C)(C)OC2=CC=C(C(C)=O)C=C2[C@@H]1NC(C3=CC(Cl)=C(F)C=C3)=O |
11 Publications Citing Use of MCE
- [1]Nature. 2016 May 18;533(7604):493-8.
- [2]Neurotherapeutics. 2017 Oct;14(4):1148-1165.
- [3]Int J Mol Sci. 2021, 22(1), 298.
- [4]Exp Eye Res. 2021 Jan;202:108384.
- [5]PLoS One. 2019 Oct 21;14(10):e0224130.
- [6]Cell Biol Int. 2021 Oct 31.
- [7]Patent. US20220280473A1.
- [8]The University of Auckland. Department of Ophthalmology Centre of Brain & Research. 2022 Jul.
- [9]Patent. US20200085781A1
- [10]Patent. US20170258758A1.
- [11]Department of Ophthalmology. Faculty of Medical and Health Sciences. The University of Auckland. 2016.
Summary
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Treatment with Tonabersat (10 mg/kg) significantly inhibits progression of metastatic lesions. Addition of NSC 241240 to either agent profoundly inhibits brain metastasis [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00332007 | Minster Research Ltd|University of Copenhagen |
Migraine With Aura
|
May 2006 | Phase 2 |
| NCT00534560 | Minster Research Ltd |
Migraine Without Aura|Migraine With Aura
|
October 2007 | Phase 2 |
| NCT00311662 | Minster Research Ltd |
Migraine Without Aura|Migraine With Aura
|
April 2006 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 255.22 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5522 mL | 12.7610 mL | 25.5219 mL |
| 5 mM | 0.5104 mL | 2.5522 mL | 5.1044 mL |
| 10 mM | 0.2552 mL | 1.2761 mL | 2.5522 mL |
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.
- [2] Chen Q, et al. Carcinoma-astrocyte gap junctions promote brain metastasis by cGAMP transfer. Nature. 2016 May 18;533(7604):493-8.
- [3] Kim Y, et al. Tonabersat Prevents Inflammatory Damage in the Central Nervous System by Blocking Connexin43 Hemichannels. Neurotherapeutics. 2017 May 30.
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