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A 839977
$104 – $660
Products Details
Product Description
– A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta[1].
Web ID
– HY-13954
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– COVID-19-immunoregulation
Molecular Formula
– C19H14Cl2N6O
References
– [1]Albalawi F et.al, The P2X7 Receptor Primes IL-1β and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain. Front Cell Neurosci. 2017 Aug 8;11:227|[2]Falk S et al.P2X7 receptor-mediated analgesia in cancer-induced bone pain. Neuroscience. 2015 Apr 16; 291:93-105.|[3]Honore P, et al. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav Brain Res. 2009 Dec 1;204(1):77-81.
CAS Number
– 870061-27-1
Molecular Weight
– 413.26
Compound Purity
– 98.74
SMILES
– ClC1=C(Cl)C(N2N=NN=C2NCC3=CC=CC=C3OC4=NC=CC=C4)=CC=C1
Clinical Information
– No Development Reported
Research Area
– Neurological Disease; Inflammation/Immunology
Solubility
– DMSO : 100 mg/mL (ultrasonic)
Target
– P2X Receptor
Isoform
– P2X7 Receptor
Pathway
– Membrane Transporter/Ion Channel
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
