GSK1014802(CNV1014802)
(Synonyms: GSK-1014802; CNV1014802) 目录号 : GC10234
GSK1014802(CNV1014802) (GSK-1014802)是一种新型的小分子状态依赖性钠通道阻滞剂； Nav1.7 钠通道抑制剂。
Cas No.:934240-30-9
Sample solution is provided at 25 µL, 10mM.
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GSK1014802 (CNV1014802) is a novel sodium channel blocker [1][2][3].
Voltage-gated sodium channels (Navs) are transmembrane ion channel proteins, which are involved in Na+ ion conduction across cell membranes during cell membrane depolarization [2].
GSK1014802 (CNV1014802) is a novel sodium channel blocker and is an effective anticonvulsant agent. In rats, GSK1014802 (20 - 80 mg/kg p.o.) attenuated the deficit in reversal learning induced by phencyclidine (PCP) in a dose-dependent way, which suggested the potential of GSK1014802 in the treatment of cognitive symptoms of schizophrenia. GSK2 was also a potent inhibitor of human MAO-B with pIC50 value of 7.96 but did not inhibit human MAO-A. GSK2 inhibited rat forebrain MAO-B with pKi value of 7.20 [1]. CNV1014802 inhibited sodium channels in a state-dependent way. CNV1014802 exhibited selectivity for the Nav1.7 subtype over the other subtypes (Nav1.1, Nav1.2, Nav1.3, Nav1.5, Nav1.6 and TTX-R) [2].
GSK1014802 had completed Phase II trials for lumbosacral radiculopathy and was in phase II trials for trigeminal neuralgia (TN). Furthermore, CNV1014802 was granted orphan drug designation in 2013 by FDA for the treatment of trigeminal neuralgia [3].
References:
[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.
| Cas No. | 934240-30-9 | SDF | |
| 别名 | GSK-1014802; CNV1014802 | ||
| 化学名 | (2S,5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carbimidic acid | ||
| Canonical SMILES | FC1=CC=CC=C1COC2=CC=C([C@@](N3)([H])CC[C@@]3([H])C(O)=N)C=C2 | ||
| 分子式 | C18H19FN2O2 | 分子量 | 314.35 |
| 溶解度 | DMSO : 83 mg/mL (264.04 mM; Need ultrasonic and warming) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1812 mL | 15.9058 mL | 31.8117 mL |
| 5 mM | 0.6362 mL | 3.1812 mL | 6.3623 mL |
| 10 mM | 0.3181 mL | 1.5906 mL | 3.1812 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet