Mirogabalin|1138245-13-2|(DS5565)-陌孚医药/Medlife

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Mirogabalin (Synonyms: DS5565)

目录号: PL02833 纯度: ≥99%

CAS No. :1138245-13-2

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中文名称	Mirogabalin
中文别名	Mirogabalin
英文名称	Mirogabalin
英文别名	Mirogabalin;2-[(1R,5S,6S)-6-(aminomethyl)-3-ethyl-6-bicyclo[3.2.0]hept-3-enyl]acetic acid;DS5565;Mirogabalin(DS-5565);(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-ene-6-acetic acid;A 200-0700;DS 5565;S7LK2KDM5U;2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid;Bicyclo[3.2.0]hept-3-ene-6-acetic acid, 6-(aminomethyl)-3-ethyl-, (1R,5S,6S)-;Bicyclo(3.2.0)hept-3-ene-6-acetic acid, 6-(aminomethyl)-3-ethyl-, (1R,5S,6S)-;((1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo(3.2.0)hept-3-en-6-yl)acetic acid;Mirogabalin [INN];Mirogabalin [USAN:INN];[(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid;DS 556
Cas No.	1138245-13-2
分子式	C₁₂H₁₉NO₂
分子量	209.28
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Mirogabalin (DS-5565)是一种选择性的 α2δ-1 配体，高效且选择性地作用于电压敏感性钙通道复合体的 α2δ-1 亚基。

生物活性

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.

性状

Solid

IC50 & Target[1][2]

α2δ-1 Calcium Channel

体外研究(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. Mirogabalin (DS-5565) is an α2δ-1 ligand being developed for pain associated with diabetic peripheral neuropathy, fibromyalgia, and posth

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: H₂O : 7.71 mg/mL (36.84 mM; Need ultrasonic)DMSO : < 1 mg/mL (insoluble or slightly soluble)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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