Mirogabalin (Synonyms: DS5565)

Name: Mirogabalin
Brand: MedChemExpress
SKU: HY-12650
Rating: 5.0 (5 reviews)

Cat. No.: HY-12650 Pureza: 99.22%: Ficha de datos
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Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.

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Mirogabalin Estructura química

No. CAS : 1138245-13-2

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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:

Mirogabalin besylate In-stock
(rel)-Mirogabalin Obtener un presupuesto
Mirogabalin-¹³C₂,d₁ (Mixture of Diastereomers) Obtener un presupuesto
Mirogabalin-d₄ Obtener un presupuesto
Mirogabalin (Standard) Obtener un presupuesto

5 Publications Citing Use of MCE Mirogabalin

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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
Pureza y Documentación
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Revisión del cliente

Descripciòn

IC₅₀ & Target

α2δ-1 Calcium Channel^[1]

In Vitro

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the central nervous system (CNS). In vitro experiments using membrane preparations from human and rat α2δ subunit-expressed cells show that Mirogabalin had a slower dissociation rate from α2δ-1 than α2δ-2, in particular, α2δ-1 compared with Pregabalin. Additionally, Mirogabalin shows potent, sustained analgesic effects in streptozotocin-induced diabetic rats with induces pain, and the superior analgesic effects and wider CNS safety margin relative to Pregabalin are attributed to its selectivity for and slow dissociation from α2δ-1 compared with Pregabalin^[1]. Mirogabalin (DS-5565) is an α2δ-1 ligand being developed for pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia. Mirogabalin targets α2δ-1, an auxiliary protein associated with voltage-sensitive calcium channel complexes in the central nervous system. This binding reduces calcium influx at nerve terminals, therefore reducing the release of several pain neurotransmitters. The ED₅₀ (on the transformed scale) for Mirogabalin is estimated to be 20.5 mg with a 90% confidence interval (CI) of 10.1-41.7 mg^[2].

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

In Vivo

Additionally, Mirogabalin shows potent, sustained analgesic effects in streptozotocin-induced diabetic rats with induced pain, and the superior analgesic effects and wider central nervous system (CNS) safety margin relative to Pregabalin are attributed to its selectivity for and slow dissociation from α2δ-1 compared with Pregabalin^[1].

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

Peso molecular

209.28

Fòrmula

C₁₂H₁₉NO₂

No. CAS

1138245-13-2

Appearance

Solid

Color

Light yellow to light brown

SMILES

O=C(O)C[C@]1(CN)[C@]2([H])C=C(CC)C[C@]2([H])C1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

H₂O : 7.71 mg/mL (36.84 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.7783 mL	23.8914 mL	47.7829 mL
5 mM	0.9557 mL	4.7783 mL	9.5566 mL
10 mM	0.4778 mL	2.3891 mL	4.7783 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, 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 0.83 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.83 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 10 mg/mL (47.78 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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: 99.22%

Select Batch:

Ficha de datos (276 KB) SDS (393 KB)

COA (249 KB) HNMR (180 KB) LCMS (96 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Vinik A, et al. Efficacy and safety of Mirogabalin (DS-5565) for the treatment of diabetic peripheral neuropathic pain: a randomized, double-blind, placebo- and active comparator-controlled, adaptive proof-of-concept phase 2 study. Diabetes Care. 2014 Dec [Content Brief]

[2]. Hutmacher MM, et al. Exposure-response modeling of average daily pain score, and dizziness and somnolence, forMirogabalin (DS-5565) in patients with diabetic peripheral neuropathic pain. J Clin Pharmacol. 2016 Jan;56(1):67-77. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	4.7783 mL	23.8914 mL	47.7829 mL	119.4572 mL
	5 mM	0.9557 mL	4.7783 mL	9.5566 mL	23.8914 mL
	10 mM	0.4778 mL	2.3891 mL	4.7783 mL	11.9457 mL
	15 mM	0.3186 mL	1.5928 mL	3.1855 mL	7.9638 mL
	20 mM	0.2389 mL	1.1946 mL	2.3891 mL	5.9729 mL
	25 mM	0.1911 mL	0.9557 mL	1.9113 mL	4.7783 mL
	30 mM	0.1593 mL	0.7964 mL	1.5928 mL	3.9819 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Mirogabalin Related Classifications

Neurological Disease

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:

Mirogabalin1138245-13-2DS5565DS 5565DS-5565Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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Mirogabalin (Synonyms: DS5565)

Revisión del cliente

Other Forms of Mirogabalin:

Mirogabalin Related Antibodies

5 Publications Citing Use of MCE Mirogabalin

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Calcium Channel:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Mirogabalin Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Mirogabalin Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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SAFETY DATA SHEET (SDS)

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