A-803467 - Sodium Channel 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEA-803467Cat. No.: HY-11079CAS No.: 944261-79-4分式: CHClNO分量: 357.79作靶点: Sodium Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (139.75 mM

2、; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7949 mL 13.9747 mL 27.9494 mL5 mM 0.5590 mL 2.7949 mL 5.5899 mL10 mM 0.2795 mL 1.3975 mL 2.7949 mL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，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液

3、可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.99 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.99 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 A

4、803467Nav1.8钠离通道阻断剂，IC50为8 nM，对Nav1.2，1.3，1.5和1.7的抑制性100倍。REFERENCES1. McGaraughty, et al. A selective NaV1.8 sodium channel blocker, A-803467 5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide), attenuates spinal neuronal activity in neuropathic rats. Journal of Pharmacology and Experimen

5、tal Therapeutics (2008),2. Jarvis MF, et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in therat. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5.3. Joshi SK, et al. Additive antinociceptive effects of the selective Nav1.8 block

6、er A-803467 and selective TRPV1 antagonists in ratinflammatory and neuropathic pain models. /pubmed/190705484. Kort ME, et al. Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 40