A-803467 - Sodium Channel 抑制劑 - 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作靶點(diǎn): Sodium Channel作通路: Membrane Transporter/Ion Channel儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (139.75 mM

2、; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液

3、可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.99 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.99 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 A

4、803467Nav1.8鈉離通道阻斷劑，IC50為8 nM，對(duì)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