A 887826
(Synonyms: 5-(4-丁氧基-3-氯苯基)-N-[[2-(4-吗啉)-3-吡啶基]甲基]-3-吡啶甲酰胺) 目录号 : GC14481
A 887826 是一种有效的、选择性的、口服生物利用度和电压依赖性 Na(v)1.8 钠通道阻滞剂，IC50 为 11 nM。
Cas No.:1266212-81-0
Sample solution is provided at 25 µL, 10mM.
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A 887826 is a potent and voltage-dependent Nav1.8 sodium channel blocker. It blocked recombinant human Nav1.8 channels with an IC50 value of 11nM [1].
Voltage-gated sodium channels are important in the generation and propagation of action potential. At least 9 genes encode functional sodium channels, namely Nav1.1-Nav1.9. Nav1.8 is a TTX-resistant (TTX-R) sodium channel. Nav1.8 is highly localized on primary sensory afferent neurons. Nav1.8 is involved in the processing of nociceptive information.
-100 mV without prepulse did make a resting state for rat DRG neurons. Prepulse to -40 mV did make an inactivated state for channels. In rat DRG neurons in these two states, treatment with A 887826 at 1 µM significantly blocked TTXR Na+ currents. A 887826 blocked TTX-R Na+ currents with an IC50 value of 7.9 ± 0.2 nM (n= 5~9) when channels were in an inactivated state (-40 mV). A 887826 showed an IC50 value of 63.6 ± 0.2 nM (n=5~9) to less depolarized (at -60, -80 or -100 mV) TTX-R Na+ currents. That meant A 887826 state-dependently blocked TTX-R Na+ currents [1].
Knockdown of Nav1.8 caused a significant reduction in mechanical hyperalgesia and allodynia in rat models of inflammatory and neuropathic pain. Suppression of Nav1.8 expression also reduced visceral pain in several experimental models. Activation of Nav1.8 sodium channels primarily drove nociceptor excitability under cold conditions. A rat spinal nerve ligation model of neuropathic pain was used. Oral administration with A 887826 dose-dependently attenuated tactile allodynia in this pain model. The range of free plasma concentrations of A 887826 to produce analgesic efficacy in a spinal nerve ligation model was 3-10 nM. This was consistent with the IC50 value for blocking rat DRG TTX-R sodium currents [1].
Reference:
[1]. Zhang XF, Shieh CC, Chapman ML, et al. A-887826 is a structurally novel, potent and voltage-dependent NaV1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats. Neuropharmacology, 2010, 59(3): 201-207.
| Cas No. | 1266212-81-0 | SDF | |
| 别名 | 5-(4-丁氧基-3-氯苯基)-N-[[2-(4-吗啉)-3-吡啶基]甲基]-3-吡啶甲酰胺 | ||
| 化学名 | 5-(4-butoxy-3-chlorophenyl)-N-((2-morpholinopyridin-3-yl)methyl)nicotinamide | ||
| Canonical SMILES | ClC1=CC(C2=CN=CC(C(NCC3=CC=CN=C3N4CCOCC4)=O)=C2)=CC=C1OCCCC | ||
| 分子式 | C26H29ClN4O3 | 分子量 | 480.99 |
| 溶解度 | <24.05mg/ml in DMSO | 储存条件 | Store at RT |
| 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 | 2.079 mL | 10.3952 mL | 20.7905 mL |
| 5 mM | 0.4158 mL | 2.079 mL | 4.1581 mL |
| 10 mM | 0.2079 mL | 1.0395 mL | 2.079 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet