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A 839977

CAT: 0804-HY-13954-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-13954-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
870061-27-1
UNSPSC
12352005
Target
P2X Receptor
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel
Applications
COVID-19-immunoregulation
Field of Research
Neurological Disease; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/a-839977.html
Purity
98.74
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
ClC1=C(Cl)C(N2N=NN=C2NCC3=CC=CC=C3OC4=NC=CC=C4)=CC=C1
Molecular Formula
C19H14Cl2N6O
Molecular Weight
413.26
References & Citations
[1]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.|[2]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|[3]Falk S et al.P2X7 receptor-mediated analgesia in cancer-induced bone pain. Neuroscience. 2015 Apr 16; 291:93-105.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
P2X7 Receptor

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