1. Membrane Transporter/Ion Channel
  2. Calcium Channel

Mirogabalin besylate (Synonyms: DS 5565 besylate)

Cat. No.: HY-108006 Purity: >98.0%
Handling Instructions

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.

Mirogabalin besylate Chemical Structure

Mirogabalin besylate Chemical Structure

CAS No. : 1138245-21-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
100 mg USD 810 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

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]

In Vitro

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].

In Vivo

Mirogabalin besylate (3 and 10 mg/kg) markedly increases AUC0-8 hours values in a dose-dependent manner in partial sciatic nerve ligation model rats. Mirogabalin (2.5, 5, and 10 mg/kg) causes significant and dose-dependent increase in AUC0-12 hours values and enhances analgesic effects, with estimated ED50 of 4.4, 3.1, and <2.5 mg/kg on day 1, day 3, and day 5, respectively. Moreover, Mirogabalin besylate shows no obvious effect on rota-rod performance and locomotor activity at 3 and 10 mg/kg via oral administration, exhibits significant inhibition on rota-rod performance at 10, 30, and 100 mg/kg, and decreases locomotor activity at 30 and 100 mg/kg in rats[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 155 mg/mL (421.81 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.58 mg/mL (7.02 mM); Clear solution

  • 3.

    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

References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

367.46

Formula

C₁₈H₂₅NO₅S

CAS No.

1138245-21-2

SMILES

O=S(C1=CC=CC=C1)(O)=O.OC(C[[email protected]@]2([[email protected]@]3([H])[[email protected]@](CC(CC)=C3)([H])C2)CN)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Mirogabalin besylate
Cat. No.:
HY-108006
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Mirogabalin besylate

Cat. No.: HY-108006