| CAS NO: | 14663-23-1 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 100mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 336.23 |
| Cas No. | 14663-23-1 |
| Formula | C14H9N4NaO5 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥12.2 mg/mL in DMSO |
| Chemical Name | sodium (E)-1-(((5-(4-nitrophenyl)furan-2-yl)methylene)amino)-4-oxo-4,5-dihydro-1H-imidazol-2-olate |
| Canonical SMILES | O=C1N=C(N(C1)/N=C/C2=CC=C(C(C=C3)=CC=C3[N+]([O-])=O)O2)[O-].[Na+] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Dantrolene (sodium salt) is an antagonist of ryanodine receptor (RyR), with an IC50 of 5.9 ± 0.3 nM for RyR2 [1, 2].
RyRs are expressed on the surface of the endoplasmic reticulum and the sarcoplasmic reticulum, responsible for Ca2+ release from intracellular stores. Dysfunction of calcium homeostasis may lead to ischemia, hypoxia, seizure, trauma, anesthesia, and neurodegenerative diseases [1].
In mouse cardiomyocytes, dantrolene showed no effect on cardiac Ca2+ release in the absence of calmodulin, but reduced Ca2+ wave frequency (IC50 = 0.42 ± 0.18 μM,Emax = 47 ± 4%) and amplitude (IC50 = 0.19 ± 0.04 μM,Emax = 66 ± 4%) in the presence of 100 nM calmodulin, which implied that calmodulin was essential for dantrolene’s inhibition on RyRs [2].
In a mouse pancreatitis model induced by caerulein for 1 hour, dantrolene (5 mg/kg) reduced pancreatic trypsin activity by 59% and mitigated early ultrastructural derangements within the acinar cell. Eight hours after caerulein induction, dantrolene decreased pancreatic trypsin activity and serum amylase by 61 and 32%, respectively [3].
References:
[1]. Inan S, Wei H. The cytoprotective effects of dantrolene: a ryanodine receptor antagonist. Anesthesia & Analgesia, 2010, 111(6): 1400-1410.
[2]. Oo Y W, Gomez-Hurtado N, Walweel K, et al. Essential Role of Calmodulin in RyR Inhibition by Dantrolene. Molecular Pharmacology, 2015, 88(1): 57-63.
[3]. Orabi A I, Shah A U, Ahmad M U, et al. Dantrolene mitigates caerulein-induced pancreatitis in vivo in mice. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2010, 299(1): G196-G204.
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