A-867744

• CAT Number: I000063
• CAS Number: 1000279-69-5
• Molecular Formula: C20H19ClN2O3S
• Molecular Weight: 402.89
• Purity: ≥95%
• Target: AChR
• Solubility: in DMSO > 10 mM
• Storage: Store at -20°C
• IC50: ~ 1 uM
• IUPAC Name: 4-[5-(4-chlorophenyl)-2-methyl-3-propanoylpyrrol-1-yl]benzenesulfonamide
• InChI: InChI=1S/C20H19ClN2O3S/c1-3-20(24)18-12-19(14-4-6-15(21)7-5-14)23(13(18)2)16-8-10-17(11-9-16)27(22,25)26/h4-12H,3H2,1-2H3,(H2,22,25,26)
• InChIKey: ABACVOXFUHDKNZ-UHFFFAOYSA-N
• SMILES: CCC(=O)C1=C(N(C(=C1)C2=CC=C(C=C2)Cl)C3=CC=C(C=C3)S(=O)(=O)N)C

A-867744（Cat No.:I000063） is a compound that acts as a positive allosteric modulator of α7 nicotinic acetylcholine receptors (nAChRs). It has been shown to have an IC50 value of 0.98 μM for human α7 receptors and 1.12 μM for rat α7 receptors, in Xenopus laevis oocytes. Notably, A-867744 does not display any activity at 5-HT3A, α3β4, or α4β2 nAChRs. These findings suggest that A-867744 may have potential therapeutic uses in conditions that involve dysfunction of α7 nAChRs, such as Alzheimer’s disease and schizophrenia.

Reference

1:Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. Faghih R, Gopalakrishnan SM, Gronlien JH, Malysz J, Briggs CA, Wetterstrand C, Ween H, Curtis MP, Sarris KA, Gfesser GA, El-Kouhen R, Robb HM, Radek RJ, Marsh KC, Bunnelle WH, Gopalakrishnan M.J Med Chem. 2009 May 28;52(10):3377-84. doi: 10.1021/jm9003818. PMID: 19419141 2:In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile. Malysz J, Grønlien JH, Anderson DJ, Håkerud M, Thorin-Hagene K, Ween H, Wetterstrand C, Briggs CA, Faghih R, Bunnelle WH, Gopalakrishnan M.J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. doi: 10.1124/jpet.109.151886. Epub 2009 Apr 23. PMID: 19389923 Free Article