Mirogabalin  ≥99%

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沸点:357.5±15.0 °C(Predicted)
密度:1.104±0.06 g/cm3(Predicted)
包装规格:1mg 5mg 25mg 100mg in glass bottle
产品简介: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。
溶解性:DMSO :< 1 mg/mL (insoluble or slightly soluble) Water:7.71 mg/mL (36.84 mM; 超声助溶)
储备液保存:-80°C, 2 years -20°C, 1 year
体内实验:1、请依序添加每种溶剂: 10% DMSO→40% PEG300→5% Tween-80→45% Saline Solubility: ≥ 0.83 mg/mL (3.97 mM); 澄清溶液 此方案可获得 ≥ 0.83 mg/mL(饱和度未知)的澄清溶液。 以 1 mL 工作液为例,取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL。 2、请依序添加每种溶剂: 10% DMSO→90% (20% SBE-β-CD in Saline) Solubility: ≥ 0.83 mg/mL (3.97 mM); 澄清溶液 此方案可获得 ≥ 0.83 mg/mL(饱和度未知)的澄清溶液。 以 1 mL 工作液为例,取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。 3、请依序添加每种溶剂: 10% DMSO→90% Corn Oil Solubility: ≥ 0.83 mg/mL (3.97 mM); 澄清溶液 此方案可获得 ≥ 0.83 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。 以 1 mL 工作液为例,取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 注:建议现用现配,在短期内尽快用完。 4、请依序添加每种溶剂: PBS Solubility: 10 mg/mL (47.78 mM); 澄清溶液; 超声助溶 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
靶点:α2δ-1 Calcium Channel
体外研究: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 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.
体内研究: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.
保存条件:-20°C
注意事项:1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。