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A-867744 CAS: 1000279-69-5

Category: Inhibitors
Product Name: A-867744
Cat No: I000063
CAS No: 1000279-69-5
Synonyms: 4-[5-(4-chlorophenyl)-2-methyl-3-propanoylpyrrol-1-yl]benzenesulfonamide
Molecular Formula: C20H19ClN2O3S
Molecular Weight: 402.89
SMILES: O=S(C1=CC=C(N2C(C)=C(C(CC)=O)C=C2C3=CC=C(Cl)C=C3)C=C1)(N)=O
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)
Solubility: in DMSO > 10 mM
Target: AChR
IC50: ~ 1 uM
Storage: Store at -20°C
CAS 1000279-69-5,A-867744
  • Description

A-867744 is a positive allosteric modulator of α7 nAChRs (IC50 values are 0.98 and 1.12 μM for human and rat α7 receptor ACh-evoked currents respectively, in X. laevis oocytes). Displays no activity at 5-HT3A, α3β4 or α4β2 nAChRs.
IC50 value: ~ 1 uM
Target: α7 nAChR

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References

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

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