A potent and selective competitive antagonist of the P2X7 receptor
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A-804598

Item No. 20060

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-cyano-N''-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine
CAS Number
1125758-85-1
Molecular Formula
C19H17N5
Formula Weight
315.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml
λmax
226, 304, 317 nm
SMILES
C[C@H](N/C(NC#N)=N\C1=CC=CC2=C1C=CC=N2)C3=CC=CC=C3
InChi Code
InChI=1S/C19H17N5/c1-14(15-7-3-2-4-8-15)23-19(22-13-20)24-18-11-5-10-17-16(18)9-6-12-21-17/h2-12,14H,1H3,(H2,22,23,24)/t14-/m0/s1
InChi Key
PQYCRDPLPKGSME-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    A-804598 is a potent and selective competitive antagonist of the purinergic P2X7 receptor, a ligand-gated ion channel, with IC50 values of 9.9 and 10.9 nM in 132N1 cells transfected with the rat or mouse receptor, respectively.1 It inhibits IL-1β release in human THP-1 cells stimulated with LPS and IFN-γ (IC50 = 8.5 nM). A-804598 is selective for P2X7 receptors over other P2X and P2Y receptors at concentrations up to 100 µM and over many G protein-coupled receptors, enzymes, transporters, and ion channels. A-804598 (25 mg/kg) prevents footshock-induced increases in IL-1β mRNA in the paraventricular nucleus of the rat hypothalamus.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Donnelly-Roberts, D.L., Namovic, M.T., Surber, B., et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology 56(1), 223-229 (2009).

    2. Cantazaro, J.M., Hueston, C.M., Deak, M.M., et al. The impact of the P2X7 receptor antagonist A-804598 on neuroimmune and behavioral consequences of stress. Behav. Pharmacol. 25(5-6), 582-598 (2014).