A P2X7 receptor allosteric modulator
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GW 791343

Item No. 32882

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(3,4-difluorophenyl)amino]-N-[2-methyl-5-(1-piperazinylmethyl)phenyl]-acetamide, dihydrochloride
CAS Number
1019779-04-4
Molecular Formula
C20H24F2N4O • 2HCl
Formula Weight
447.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 1 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
235 nm
SMILES
O=C(CNC1=CC=C(C(F)=C1)F)NC2=CC(CN3CCNCC3)=CC=C2C.Cl.Cl
InChi Code
InChI=1S/C20H24F2N4O.2ClH/c1-14-2-3-15(13-26-8-6-23-7-9-26)10-19(14)25-20(27)12-24-16-4-5-17(21)18(22)11-16;;/h2-5,10-11,23-24H,6-9,12-13H2,1H3,(H,25,27);2*1H
InChi Key
IYJPZTBIYHPSKF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    25 mg

    $219

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    50 mg

    $392

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    100 mg

    $696

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    Product Description

    GW 791343 is an allosteric modulator of the purinergic P2X7 receptor.1 It acts as a negative allosteric modulator at human P2X7 receptors but as a positive allosteric modulator at rat P2X7 receptors. GW 791343 (10 and 30 µM) reduces ethidium accumulation induced by the P2X receptor agonists ATP (Item No. 14498) or BzATP (Item No. 15577) in HEK293 cells expressing the human receptor. In contrast, it increases ethidium accumulation induced by ATP or BzATP in HEK293 cells expressing the rat receptor when used at the same concentrations. GW 791343 (5 µM) potentiates the circadian release of ATP in rat organotypic suprachiasmatic nucleus (SCN) slice cultures.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Michel, A.D., Chambers, L.J., and Walter, D.S. Negative and positive allosteric modulators of the P2X7 receptor. Br. J. Pharmacol. 153(4), 737-750 (2008).

    2. Svobodova, I., Bhattaracharya, A., Ivetic, M., et al. Circadian ATP Release in Organotypic Cultures of the Rat Suprachiasmatic Nucleus Is Dependent on P2X7 and P2Y Receptors. Front. Pharmacol. 9, 192 (2018).