A positive allosteric modulator of AMPA receptors
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LY404187

Item No. 28741

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(4′-cyano[1,1′-biphenyl]-4-yl)propyl]-2-propanesulfonamide
CAS Number
211311-95-4
Molecular Formula
C19H22N2O2S
Formula Weight
342.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 15mg/mLDMSO: 15mg/mLDMSO:PBS (pH 7.2) (1:4): 0.2mg/mLEthanol: 3mg/mL
λmax
278 nm
SMILES
CC(CNS(C(C)C)(=O)=O)C(C=C1)=CC=C1C2=CC=C(C#N)C=C2
InChi Code
InChI=1S/C19H22N2O2S/c1-14(2)24(22,23)21-13-15(3)17-8-10-19(11-9-17)18-6-4-16(12-20)5-7-18/h4-11,14-15,21H,13H2,1-3H3
InChi Key
HOQAVGZLYRYHSO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $121

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    10 mg

    $193

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    25 mg

    $388

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    50 mg

    $597

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    Product Description

    LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.1 It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.2,3 LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Miu, P., Jarvie, K.R., Radhakrishnan, V., et al. Novel AMPA receptor potentiators LY392098 and LY404187: Effects on recombinant human AMPA receptors in vitro. Neuropharmacology 40(8), 976-983 (2001).

    2. Baumbarger, P.J., Muhlhauser, M., Zhai, J., et al. Positive modulation of α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors in prefrontal cortical pyramidal neurons by a novel allosteric potentiator. J. Pharmacol. Exp. Ther. 298(1), 86-102 (2001).

    3. Gates, M., Ogden, A., and Bleakman, D. Pharmacological effects of AMPA receptor potentiators LY392098 and LY404187 on rat neuronal AMPA receptors in vitro. Neuropharmacology 40(8), 984-991 (2001).

    4. O'Neill, M.J., Murray, T.K., Whalley, K., et al. Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson’s disease. Eur. J. Pharmacol. 486(2), 163-174 (2004).