2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. Mirogabalin besylate

Mirogabalin besylate  (Synonyms: DS 5565 besylate)

Cat. No.: HY-108006 Pureza: 99.57%
COA
SDS
Instrucciones de manejo Technical Support

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.

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Mirogabalin besylate

Mirogabalin besylate Estructura química

No. CAS : 1138245-21-2

Tamaño Precio Stock Cantidad
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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtener un presupuesto  
500 mg   Obtener un presupuesto  

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Revisión del cliente

Based on 5 publication(s) in Google Scholar

Other Forms of Mirogabalin besylate:

Mirogabalin besylate Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas Calcium Channel:

Ver todas las isoformas
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Actividad biológica

  • Protocolo

  • Pureza y Documentación

  • Referencias

  • Revisión del cliente

Descripciòn

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].

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

Mirogabalin besylate Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
Peso molecular

367.46

Fòrmula

C18H25NO5S
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad
In Vitro: 

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)

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
View the 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.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Pureza y Documentación

Purity: 99.57%

SDS (394 KB)

COA (255 KB) LCMS (87 KB)

Instrucciones de manejo (2659 KB)
Referencias
Administraciòn de animales
[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

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
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Mirogabalin besylate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mirogabalin besylate1138245-21-2DS 5565 besylateCalcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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Mirogabalin besylate
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