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

Mirogabalin  (Synonyms: DS5565)

製品番号: HY-12650 純度: 99.22%
COA 取扱説明書 Technical Support

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

Mirogabalin 構造式

CAS 番号 : 1138245-13-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 110 在庫あり
Solution
10 mM * 1 mL in Water USD 110 在庫あり
Solid
5 mg $100 在庫あり
10 mg $155 在庫あり
25 mg $270 在庫あり
50 mg $410 在庫あり
100 mg $620 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 5 publication(s) in Google Scholar

Other Forms of Mirogabalin:

Mirogabalin 関連抗体

Top Publications Citing Use of Products

Calcium Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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製品説明

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.

IC50 & Target

α2δ-1 Calcium Channel[1]
体外実験

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.

Mirogabalin 関連抗体
体内実験

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.
分子量

209.28

分子式

C12H19NO2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

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
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g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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.
純度とドキュメンテーション

純度: 99.22%

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

取扱説明書 (2659 KB)
参考文献

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.

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.

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Mirogabalin Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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