Mirogabalin besylate
Based on 6 publication(s) in Google Scholar
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 1138245-21-2
- Formula: C18H25NO5S
- Molecular Weight:367.46
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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) Mirogabalin besylate
More- Cell Commun Signal. 2024 Feb 1;22(1):92. [Abstract]
- Brain Behav Immun. 2021 Jul:95:344-361. [Abstract]
- Pharmaceuticals (Basel). 2023 Jul 19;16(7):1023. [Abstract]
- Pharmaceuticals (Basel). 2022 Jan 13;15(1):88. [Abstract]
- Molecules. 2023 Nov 30;28(23):7862. [Abstract]
- Pharmacol Rep. 2026 May 28. [Abstract]
All Calcium Channel Isoforms
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Biological Activity
Kd: 13.5 nM (Human α2δ-1), 22.7 nM (Human α2δ-2), 27 nM (Rat α2δ-1), 47.6 nM (Rat α2δ-2)[1]
Mirogabalin besylate is a ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively. Mirogabalin shows binding affinity for the gabapentin binding site in rat cortical brain homogenates with the IC50 value of 16.0 nM. Mirogabalin has no effect on any other receptors, channels, transporters, or enzymes at 50 μM[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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1138245-21-2
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Appearance Solid
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Molecular Weight 367.46
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Formula C18H25NO5S
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Color White to off-white
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SMILES
O=S(C1=CC=CC=C1)(O)=O.OC(C[C@@]2([C@@]3([H])[C@@](CC(CC)=C3)([H])C2)CN)=O
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Synonyms
DS 5565 besylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
T-type voltage-gated channels, Na+/Ca2+-exchanger, and calpain-2 promote photoreceptor cell death in inherited retinal degeneration. [Abstract]2024 Feb 1;22(1):92. PMID: 38303059 -
Brain Behav Immun
Microglial IL-10 and β-endorphin expression mediates gabapentinoids antineuropathic pain. [Abstract]2021 Jul:95:344-361. PMID: 33862171 -
Pharmaceuticals (Basel)
Mirogabalin Decreases Pain-like Behaviors by Inhibiting the Microglial/Macrophage Activation, p38MAPK Signaling, and Pronociceptive CCL2 and CCL5 Release in a Mouse Model of Neuropathic Pain. [Abstract]2023 Jul 19;16(7):1023. PMID: 37513935 -
Pharmaceuticals (Basel)
Mirogabalin Decreases Pain-like Behaviours and Improves Opioid and Ketamine Antinociception in a Mouse Model of Neuropathic Pain. [Abstract]2022 Jan 13;15(1):88. PMID: 35056145 -
Molecules
Naturally Inspired Molecules for Neuropathic Pain Inhibition-Effect of Mirogabalin and Cebranopadol on Mechanical and Thermal Nociceptive Threshold in Mice. [Abstract]2023 Nov 30;28(23):7862. PMID: 38067591 -
Pharmacol Rep
Therapeutic potential of combining mirogabalin with antidepressants in relieving hypersensitivity: evidence from a mouse model of neuropathic pain. [Abstract]2026 May 28. PMID: 42207469
Solvent & Solubility
DMSO : 100 mg/mL (272.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.58 mg/mL (7.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.58 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 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: ≥ 2.58 mg/mL (7.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.58 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Rats[1]
Eighty male rats are divided into groups of eight. After oral administration of Mirogabalin besylate (1, 3, 10, 30, and 100 mg/kg) or vehicle (control), locomotor activity is measured for 1 hour using the SUPERMEX system. Based on the time of peak effects of the test compounds (Mirogabalin besylate, etc.) in the rota-rod test, the pretreatment time is set at 6 hours for mirogabalin besylate and at 4 hours for pregabalin[1].
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 (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7214 mL | 13.6069 mL | 27.2138 mL | 68.0346 mL |
| 5 mM | 0.5443 mL | 2.7214 mL | 5.4428 mL | 13.6069 mL | |
| 10 mM | 0.2721 mL | 1.3607 mL | 2.7214 mL | 6.8035 mL | |
| 15 mM | 0.1814 mL | 0.9071 mL | 1.8143 mL | 4.5356 mL | |
| 20 mM | 0.1361 mL | 0.6803 mL | 1.3607 mL | 3.4017 mL | |
| 25 mM | 0.1089 mL | 0.5443 mL | 1.0886 mL | 2.7214 mL | |
| 30 mM | 0.0907 mL | 0.4536 mL | 0.9071 mL | 2.2678 mL | |
| 40 mM | 0.0680 mL | 0.3402 mL | 0.6803 mL | 1.7009 mL | |
| 50 mM | 0.0544 mL | 0.2721 mL | 0.5443 mL | 1.3607 mL | |
| 60 mM | 0.0454 mL | 0.2268 mL | 0.4536 mL | 1.1339 mL | |
| 80 mM | 0.0340 mL | 0.1701 mL | 0.3402 mL | 0.8504 mL | |
| 100 mM | 0.0272 mL | 0.1361 mL | 0.2721 mL | 0.6803 mL |
Mirogabalin besylate Related Classifications
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