产品
编 号:F291833
分子式:C14H16N4NaO8.5
分子量:399.31
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10mM*1mL in DMSO
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100mg
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500mg
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生物活性:
Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.

体内研究:
Dantrolene (5 mg/kg;每周口服两次) sodium hemiheptahydrate 可改善平衡木行走和步态行走测定中的表现。 Dantrolene (10mg/kg;腹腔;每周三天;持续 40-60 天) sodium hemiheptahydrate 可显着改善步态,降低 LC3-II 水平,改善线粒体 ATP 生成并减少大脑炎症。Dantrolene sodium hemiheptahydrate 降低神经病性戈谢病小鼠大脑中的自噬和 CALM (钙调蛋白)的表达。 Animal Model:YAC128 transgenic mice (FVBN/NJ background strain) and WT mice
Dosage:5 mg/kg
Administration:Fed orally twice per week from 2 to 11.5 months of age
Result:Resulted in significantly improved performance in the beam-walking and gait-walking assays. Significantly reduced the loss of NeuN-positive striatal neurons and reduced formation of Httexp nuclear aggregates.

体外研究:
Dantrolene (60 μM;第 1 天和第 3 天) sodium hemiheptahydrate 显着抑制 paVIC 中的 ACTA2 表达并上调 RUNX2 表达。 Dantrolene (60 μM;过夜预处理) sodium hemiheptahydrate 可抑制猪主动脉瓣间质细胞中 LPC 诱导的钙流。Dantrolene (10、30、60 μM) sodium hemiheptahydrate 可抑制 10 μM 溶血磷脂酰胆碱 (LPC) 引起的 paVIC 钙化结节的形成。
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