中文名 | Azumolene |
英文名 | Azumolene EU4093 EU-4093 EU 4093 |
别名 | 阿珠莫林 |
英文别名 | EU4093 EU 4093 EU-4093 Azumolene EU4093 free base 1-[[[5-(4-Bromophenyl)-2-oxazolyl]methylene]amino]hydantoin 2,4-Imidazolidinedione, 1-[[[5-(4-bromophenyl)-2-oxazolyl]methylene]amino]- |
CAS | 64748-79-4 |
化学式 | C13H9BrN4O3 |
分子量 | 349.14 |
存储条件 | -20℃ |
体外研究 | Pretreatment with 20 µM Azumolene for 1-2 min inhibits SOCE activated by subsequent addition of caffeine and ryanodine to promote RyR-dependent sarcoplasmic reticulum Ca 2+ store depletion in mouse myotubes and adult muscle fibers. |
体内研究 | The effect of Azumolene (EU4093) on the twitch of the intact rat soleus preparation is nearly maximal at a dose of 20 mg/kg. This dose of Azumolene reduces the amplitude of the twitch to 31.9% of the control value. The contraction of intrafusal muscle as measured by the response of spindle afferent discharge is also reduced by Azumolene. |
上游原料 | 盐酸 氧氯化磷 2,4'-二溴苯乙酮 Borneol-D3 3-INDOXYL PHOSPHATE, DI-P-TOLUIDINIUM SALT 三氯氧磷 |
参考资料 展开查看 | 1: Si D, Azam MA, Lai PFH, Zamiri N, Kichigina G, Asta J, Massé S, Bokhari MM, Porta-Sánchez A, Labos C, Sun H, Yang P, Nanthakumar K. Essential role of ryanodine receptor 2 phosphorylation in the effect of azumolene on ventricular arrhythmia vulnerability in a rabbit heart model. J Cardiovasc Electrophysiol. 2018 Dec;29(12):1707-1715. doi: 10.1111/jce.13737. Epub 2018 Oct 31. PMID: 30203424. 2: Talbert EE, Smuder AJ, Kwon OS, Sollanek KJ, Wiggs MP, Powers SK. Blockage of the Ryanodine Receptor via Azumolene Does Not Prevent Mechanical Ventilation- Induced Diaphragm Atrophy. PLoS One. 2016 Feb 5;11(2):e0148161. doi: 10.1371/journal.pone.0148161. PMID: 26849371; PMCID: PMC4744044. 3: Zhao X, Min CK, Ko JK, Parness J, Kim DH, Weisleder N, Ma J. Increased store- operated Ca2+ entry in skeletal muscle with reduced calsequestrin-1 expression. Biophys J. 2010 Sep 8;99(5):1556-64. doi: 10.1016/j.bpj.2010.06.050. PMID: 20816068; PMCID: PMC2931717. 4: Zhao X, Weisleder N, Han X, Pan Z, Parness J, Brotto M, Ma J. Azumolene inhibits a component of store-operated calcium entry coupled to the skeletal muscle ryanodine receptor. J Biol Chem. 2006 Nov 3;281(44):33477-86. doi: 10.1074/jbc.M602306200. Epub 2006 Aug 31. PMID: 16945924. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.864 ml | 14.321 ml | 28.641 ml |
5 mM | 0.573 ml | 2.864 ml | 5.728 ml |
10 mM | 0.286 ml | 1.432 ml | 2.864 ml |
5 mM | 0.057 ml | 0.286 ml | 0.573 ml |
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