A positive allosteric modulator of α7 nAChRs
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A-867744

Item No. 32974

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[5-(4-chlorophenyl)-2-methyl-3-(1-oxopropyl)-1H-pyrrol-1-yl]-benzenesulfonamide
CAS Number
1000279-69-5
Molecular Formula
C20H19ClN2O3S
Formula Weight
402.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
251 nm
SMILES
CC1=C(C(CC)=O)C=C(C2=CC=C(Cl)C=C2)N1C3=CC=C(S(N)(=O)=O)C=C3
InChi Code
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)
InChi Key
ABACVOXFUHDKNZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $134

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    50 mg

    $530

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    100 mg

    $862

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    Product Description

    A-867744 is a positive allosteric modulator of α7 nicotinic acetylcholine receptors (nAChRs).1 It is selective for α7 nAChRs over α3β2- or α4β2 subunit-containing nAChRs (IC50s = 0.023, 19.5 and 6.4 µM, respectively) and the serotonin (5-HT) receptor subtype 5-HT3A (Ki = >30 µM). A-867744 potentiates ACh-induced currents in Xenopus oocytes expressing human α7 nAChRs (EC50 = ~1 µM). In vivo, A-867744 (0.1-10 μmol/kg, i.p.) improves sensory gating deficits in a paired auditory stimulus paradigm in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Malysz, J., Grønlien, J.H., Anderson, D.J., et al. In vitro pharmacological characterization of a novel allosteric modulator of α7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile. J. Pharmacol. Exp. Ther. 330(1), 257-267 (2009).

    2. Faghih, R., Gopalakrishnan, S.M., Gronlien, J.H., et al. 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 α7 nicotinic acetylcholine receptor. J. Med. Chem. 52(10), 3377-3384 (2009).