Mirogabalin (DS5565) (Synonyms: DS-5565) |
カタログ番号GC30873
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ミロガバリン (DS5565) (DS-5565) は、CNS の電位感受性カルシウムチャネル複合体の α2δ-1 サブユニットに対する高い効力と選択性を特徴とする、新規の優先的に選択的な α2δ-1 リガンドです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1138245-13-2
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
[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 [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.
| Cas No. | 1138245-13-2 | SDF | |
| 同義語 | DS-5565 | ||
| Canonical SMILES | O=C(O)C[C@]1(CN)[C@]2([H])C=C(CC)C[C@]2([H])C1 | ||
| Formula | C12H19NO2 | M.Wt | 209.28 |
| 溶解度 | Methanol : 16 mg/mL (76.45 mM);Water : 7.71 mg/mL (36.84 mM);DMSO : < 1 mg/mL (insoluble or slightly soluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.7783 mL | 23.8914 mL | 47.7829 mL |
| 5 mM | 955.7 μL | 4.7783 mL | 9.5566 mL |
| 10 mM | 477.8 μL | 2.3891 mL | 4.7783 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)