GSK1014802(CNV1014802)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GSK1014802(CNV1014802)是一种新型的钠通道阻滞剂[1][2][3].
电压门控钠通道(Navs)是跨膜的离子通道蛋白,在细胞膜去极化时,参与Na+跨膜转运[2].
GSK1014802(CNV1014802)是一种新型的钠通道阻滞剂,同时也是一种有效的抗惊厥药.在大鼠中,GSK1014802(20 ~ 80 mg/kg,口服)呈剂量依赖性地缓解Phencyclidine(PCP)诱导的逆转学习缺陷,这表明GSK1014802有望用于治疗精神分裂症的认知症状.GSK2也是一种有效的人MAO-B抑制剂,其pIC50值为7.96,但对人MAO-A无抑制作用.GSK2抑制大鼠前脑中的MAO-B,其pKi值为7.20[1].CNV1014802状态依赖性地抑制钠通道.相对于其它Nav亚型(Nav1.1\Nav1.2\Nav1.3\Nav1.5\Nav1.6以及TTX-R),CNV1014802选择性地作用于Nav1.7亚型[2].
GSK1014802已完成了治疗腰骶神经根病的II期临床试验,正处于治疗三叉神经痛(TN)的II期临床试验.此外,CNV1014802于2013年获得了美国FDA授予的用于治疗三叉神经痛的孤儿药资格[3].
参考文献：
[1]. Large CH, Bison S, Sartori I, et al. The efficacy of sodium channel blockers to prevent phencyclidine-induced cognitive dysfunction in the rat: potential for novel treatments for schizophrenia. J Pharmacol Exp Ther, 2011, 338(1): 100-113.
[2]. Bagal SK, Chapman ML, Marron BE, et al. Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett, 2014, 24(16): 3690-3699.
[3]. Zakrzewska JM, Palmer J, Ettlin DA, et al. Novel design for a phase IIa placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of CNV1014802 in patients with trigeminal neuralgia. Trials, 2013, 14: 402.
| Storage | Store at -20°C |
| M.Wt | 314.35 |
| Cas No. | 934240-30-9 |
| Formula | C18H19FN2O2 |
| Solubility | Soluble in DMSO |
| Chemical Name | (2S,5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carbimidic acid |
| SDF | Download SDF |
| Canonical SMILES | FC1=CC=CC=C1COC2=CC=C([C@@](N3)([H])CC[C@@]3([H])C(O)=N)C=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。 |
化学结构
