Tonabersat
Based on 21 publication(s) in Google Scholar
Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system.
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 175013-84-0
- Formula: C20H19ClFNO4
- Molecular Weight:391.82
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tonabersat
More- Nature. 2016 May 18;533(7604):493-8. [Abstract]
- Neurotherapeutics. 2017 Oct;14(4):1148-1165. [Abstract]
- Drug Deliv Transl Res. 2025 May 13. [Abstract]
- Int J Mol Sci. 2025 Aug 19;26(16):7996. [Abstract]
- Int J Mol Sci. 2023 Feb 15;24(4):3876. [Abstract]
- Int J Mol Sci. 2020 Dec 30;22(1):298. [Abstract]
- Eur J Pharmacol. 2026 Jan 12:1011:178442. [Abstract]
- Methods. 2024 Nov:231:178-185. [Abstract]
- Exp Neurol. 2024 Jan:371:114611. [Abstract]
- Cell Biol Int. 2022 Feb;46(2):323-330. [Abstract]
- Exp Eye Res. 2021 Jan;202:108384. [Abstract]
- PLoS One. 2024 Mar 15;19(3):e0300552. [Abstract]
- PLoS One. 2019 Oct 21;14(10):e0224130. [Abstract]
- Pharm Dev Technol. 2025 May 6:1-20. [Abstract]
- bioRxiv. 2026 May 13.
- Nanyang Technological University. 2024 Feb 17.
- Patent. US20220280473A1.
- The University of Auckland. 2022 Jul.
- Patent. US20200085781A1
- Patent. US20170258758A1.
- The University of Auckland. 2016.
Customer Validation & Images
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Cell Proliferation/Viability Assay
Biological Activity
Gap-junction[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 175013-84-0
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Appearance Solid
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Molecular Weight 391.82
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Formula C20H19ClFNO4
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Color White to yellow
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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
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Synonyms
SB-220453
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (21)
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Journal Impact Factor
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Most Recent
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Nature
2016 May 18;533(7604):493-8. PMID: 27225120 -
Neurotherapeutics
Tonabersat Prevents Inflammatory Damage in the Central Nervous System by Blocking Connexin43 Hemichannels. [Abstract]2017 Oct;14(4):1148-1165. PMID: 28560708 -
Drug Deliv Transl Res
Evaluation of ocular tolerability and bioavailability of tonabersat transfersomes ex vivo. [Abstract]2025 May 13. PMID: 40358832 -
Int J Mol Sci
2025 Aug 19;26(16):7996. PMID: 40869318 -
Int J Mol Sci
Orally Delivered Connexin43 Hemichannel Blocker, Tonabersat, Inhibits Vascular Breakdown and Inflammasome Activation in a Mouse Model of Diabetic Retinopathy. [Abstract]2023 Feb 15;24(4):3876. PMID: 36835288 -
Int J Mol Sci
Tonabersat Inhibits Connexin43 Hemichannel Opening and Inflammasome Activation in an In Vitro Retinal Epithelial Cell Model of Diabetic Retinopathy. [Abstract]2020 Dec 30;22(1):298. PMID: 33396676 -
Eur J Pharmacol
Inhibiting the NLRP3 inflammasome pathway: An effective way to treat chronic inflammation in experimental autoimmune uveitis. [Abstract]2026 Jan 12:1011:178442. PMID: 41352704 -
Methods
Development and validation of a stability-indicating HPLC method for assay of tonabersat in pharmaceutical formulations. [Abstract]2024 Nov:231:178-185. PMID: 39368764 -
Exp Neurol
Blockade of connexin hemichannels with tonabersat protects against mild hypoxic ischemic brain injury in neonatal rats. [Abstract]2024 Jan:371:114611. PMID: 37944882 -
Cell Biol Int
Blocking connexin43 hemichannels prevents TGF-β2 upregulation and epithelial-mesenchymal transition in retinal pigment epithelial cells. [Abstract]2022 Feb;46(2):323-330. PMID: 34719065 -
Exp Eye Res
Connexin43 hemichannel block inhibits NLRP3 inflammasome activation in a human retinal explant model of diabetic retinopathy. [Abstract]2021 Jan;202:108384. PMID: 33285185 -
PLoS One
Integrating and optimizing tonabersat in standard glioblastoma therapy: A preclinical study. [Abstract]2024 Mar 15;19(3):e0300552. PMID: 38489314 -
PLoS One
Adjuvant therapeutic potential of tonabersat in the standard treatment of glioblastoma: A preclinical F98 glioblastoma rat model study. [Abstract]2019 Oct 21;14(10):e0224130. PMID: 31634381 -
Pharm Dev Technol
2025 May 6:1-20. PMID: 40327409 -
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Tonabersat purchased from MedChemExpress. Usage Cited in: Patent. US20170258758A1.
ELISA of IFNα and TNFα in conditioned media from co-cultured MDA231-BrM2 cell and astrocytes in the presence of Tonabersat (Tona) with indicated concentrations.
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Solvent & Solubility
DMSO : ≥ 100 mg/mL (255.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.38 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Portuguese - PT (537 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5522 mL | 12.7610 mL | 25.5219 mL | 63.8048 mL |
| 5 mM | 0.5104 mL | 2.5522 mL | 5.1044 mL | 12.7610 mL | |
| 10 mM | 0.2552 mL | 1.2761 mL | 2.5522 mL | 6.3805 mL | |
| 15 mM | 0.1701 mL | 0.8507 mL | 1.7015 mL | 4.2537 mL | |
| 20 mM | 0.1276 mL | 0.6380 mL | 1.2761 mL | 3.1902 mL | |
| 25 mM | 0.1021 mL | 0.5104 mL | 1.0209 mL | 2.5522 mL | |
| 30 mM | 0.0851 mL | 0.4254 mL | 0.8507 mL | 2.1268 mL | |
| 40 mM | 0.0638 mL | 0.3190 mL | 0.6380 mL | 1.5951 mL | |
| 50 mM | 0.0510 mL | 0.2552 mL | 0.5104 mL | 1.2761 mL | |
| 60 mM | 0.0425 mL | 0.2127 mL | 0.4254 mL | 1.0634 mL | |
| 80 mM | 0.0319 mL | 0.1595 mL | 0.3190 mL | 0.7976 mL | |
| 100 mM | 0.0255 mL | 0.1276 mL | 0.2552 mL | 0.6380 mL |
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