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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Mirogabalin besylate (DS-5565) is a potent, selective and orally bioavailable α2δ-1 ligand under development for treating pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia. It has affinities 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 was estimated to be 17-fold more potent than pregabalin. Mirogabalin is being developed by Daiichi Sankyo and related to drugs such as gabapentin and pregabalin. Similarly to these drugs, mirogabalin binds to the α2δ calcium channels (1 and 2), but with significantly higher potency than pregabalin. It has shown promising results in Phase II clinical trials for the treatment of diabetic peripheral neuropathic pain.
| ln Vitro |
Mirogabalin besylate is a ligand for voltage-gated calcium channel's α2δ subunit. Rat α2δ-1, rat α2δ-2, human α2δ-1, and rat α2δ have Kd values of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM, in that order. is -2. In rat cortical brain homogenate, mirogabalin binds with affinity to the gabapentin binding site, with an IC50 value of 16.0 nM. At 50 μM, no additional receptors, channels, transporters, or enzymes are affected by milopalin [1].
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| ln Vivo |
Rats with a partial sciatic nerve ligation model showed a dose-dependent substantial rise in AUC0-8 hour values when treated with mirogabalin besylate (3 and 10 mg/kg). With estimated ED50s of 4.4, 3.1, and < 2.5 mg/kg, and day 5, milopalin (2.5, 5 and 10 mg/kg) resulted in a significant and dose-dependent rise in AUC0-12 hour values and increased analgesia. Furthermore, rotarod performance and locomotor activity were not significantly affected by the oral administration of milopaline besylate at 3 or 10 mg/kg, but they were considerably suppressed by the oral administration of 10, 30, and 100 mg/kg. Rats responded favorably to 30 and 100 mg/kg [1].
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| References |
[1]. Domon Y, et al. Binding Characteristics and Analgesic Effects of Mirogabalin, a Novel Ligand for the α2δ Subunit of Voltage-Gated Calcium Channels. J Pharmacol Exp Ther. 2018 Jun;365(3):573-582
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| Molecular Formula |
C18H25NO5S
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|---|---|
| Molecular Weight |
367.46
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| Exact Mass |
367.1453
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| CAS # |
1138245-21-2
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| Related CAS # |
1138245-21-2 (besylate);1138245-13-2;
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| SMILES |
InChI=1S/C12H19NO2.C6H6O3S/c1-2-8-3-9-5-12(7-13,6-11(14)15)10(9)4-87-10(8,9)6-4-2-1-3-5-6/h4,9-10H,2-3,5-7,13H2,1H3,(H,14,15)1-5H,(H,7,8,9)/t9-,10-,12-/m1./s1
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| InChi Key |
2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid compound with benzenesulfonic acid (1
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| InChi Code |
OKJXJRVWXYRSAN-TXULWXBWSA-N
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| Chemical Name |
DS-5565 DS 5565 DS5565 A-2000700 Mirogabalin Mirogabalin besylate.
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| Synonyms |
DS-5565 DS 5565 DS5565 A-2000700A2000700A 2000700
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~340.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.58 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.58 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.58 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7214 mL | 13.6069 mL | 27.2138 mL | |
| 5 mM | 0.5443 mL | 2.7214 mL | 5.4428 mL | |
| 10 mM | 0.2721 mL | 1.3607 mL | 2.7214 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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