A-803467

• CAT Number: I005620
• CAS Number: 944261-79-4
• Molecular Formula: C19H16ClNO4
• Molecular Weight: 357.8
• Purity: ≥95%
• Target: Sodium Channel
• Solubility: DMSO: >10 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 8 nM
• IUPAC Name: 5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide
• InChI: InChI=1S/C19H16ClNO4/c1-23-15-9-14(10-16(11-15)24-2)21-19(22)18-8-7-17(25-18)12-3-5-13(20)6-4-12/h3-11H,1-2H3,(H,21,22)
• InChIKey: VHKBTPQDHDSBSP-UHFFFAOYSA-N
• SMILES: COc1cc(OC)cc(c1)NC(=O)c1ccc(o1)c1ccc(Cl)cc1

A 803467 (Cat.No:I005620) is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7. A-803467 dose-dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models.

Reference

1:A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo. Anreddy N, Patel A, Zhang YK, Wang YJ, Shukla S, Kathawala RJ, Kumar P, Gupta P, Ambudkar SV, Wurpel JN, Chen ZS, Guo H.Oncotarget. 2015 Nov 17;6(36):39276-91. doi: 10.18632/oncotarget.5747. PMID: 26515463 Free PMC Article2:The effects of A-803467 on cardiac Nav1.5 channels. Han Z, Jiang Y, Xiao F, Cao K, Wang DW.Eur J Pharmacol. 2015 May 5;754:52-60. doi: 10.1016/j.ejphar.2015.02.019. Epub 2015 Feb 19. PMID: 25701724 3:Additive antinociceptive effects of the selective Nav1.8 blocker A-803467 and selective TRPV1 antagonists in rat inflammatory and neuropathic pain models. Joshi SK, Honore P, Hernandez G, Schmidt R, Gomtsyan A, Scanio M, Kort M, Jarvis MF.J Pain. 2009 Mar;10(3):306-15. doi: 10.1016/j.jpain.2008.09.007. Epub 2008 Dec 13. PMID: 19070548 4: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. McGaraughty S, Chu KL, Scanio MJ, Kort ME, Faltynek CR, Jarvis MF.J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11. Epub 2007 Dec 18. PMID: 18089840 Free Article5:A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS.Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. Epub 2007 May 2. PMID: 17483457 Free PMC Article