A 839977

P2X7 antagonist,potent and selective CAS# 870061-27-1

A 839977

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A 839977

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Chemical Properties of A 839977

Cas No. 870061-27-1 SDF Download SDF
PubChem ID 53325875 Appearance Powder
Formula C19H14Cl2N6O M.Wt 413.26
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 1-(2,3-dichlorophenyl)-N-[(2-pyridin-2-yloxyphenyl)methyl]tetrazol-5-amine
SMILES C1=CC=C(C(=C1)CNC2=NN=NN2C3=C(C(=CC=C3)Cl)Cl)OC4=CC=CC=N4
Standard InChIKey GMVNBKZQJFRFAR-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H14Cl2N6O/c20-14-7-5-8-15(18(14)21)27-19(24-25-26-27)23-12-13-6-1-2-9-16(13)28-17-10-3-4-11-22-17/h1-11H,12H2,(H,23,24,26)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of A 839977

DescriptionPotent P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively). Displays antinociceptive effects in rat and mice models of inflammatory pain. CNS penetrant.

A 839977 Dilution Calculator

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Preparing Stock Solutions of A 839977

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4198 mL 12.0989 mL 24.1978 mL 48.3957 mL 60.4946 mL
5 mM 0.484 mL 2.4198 mL 4.8396 mL 9.6791 mL 12.0989 mL
10 mM 0.242 mL 1.2099 mL 2.4198 mL 4.8396 mL 6.0495 mL
50 mM 0.0484 mL 0.242 mL 0.484 mL 0.9679 mL 1.2099 mL
100 mM 0.0242 mL 0.121 mL 0.242 mL 0.484 mL 0.6049 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on A 839977

A839977 is a novel and selective antagonist of P2X7 receptor with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively [1].

A839977 has been reported to block BzATP-evoked changes in intracellular calcium concentrations in 132N1 cells stable expressing P2X7 receptors with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively. In addition, A839977 has also revealed to inhibit BzATP-stimulated IL-1β release and YO-PRO uptake with the IC50 of 37nM and 7nM, respectively, in differentiated human THP-1 cells. Besides, A839977 has been noted to produce parallel rightward shifts in BzATP concentration-effect calcium influx curves with the pAα value of 8.1. Apart from these, A839977 has been exhibited to reduce CFA-induced thermal hyperalgesia in a dose-dependent fashion with the ED50 value of 100μmol/kg(i.p.) [1].

References:
[1] Honore P1, Donnelly-Roberts D, Namovic M, Zhong C, Wade C, Chandran P, Zhu C, Carroll W, Perez-Medrano A, Iwakura Y, Jarvis MF. 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.

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References on A 839977

The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice.[Pubmed:19464323]

Behav Brain Res. 2009 Dec 1;204(1):77-81.

The pro-inflammatory cytokine interleukin-1beta (IL-1beta) has been implicated in both inflammatory processes and nociceptive neurotransmission. Activation of P2X7 receptors is the mechanism by which ATP stimulates the rapid maturation and release of IL-1beta from macrophages and microglial cells. Recently, selective P2X7 receptor antagonists have been shown to reduce inflammatory and neuropathic pain in animal models. However, the mechanisms underlying these analgesic effects are unknown. The present studies characterize the pharmacology and antinociceptive effects of a structurally novel P2X7 antagonist. A-839977 potently (IC50=20-150 nM) blocked BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors. A-839977 also potently blocked agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells. Systemic administration of A-839977 dose-dependently reduced thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) (ED50=100 micromol/kg, i.p.) in rats. A-839977 also produced robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice (ED50=40 micromol/kg, i.p.), but the antihyperalgesic effects of A-839977 were completely absent in IL-1alphabeta knockout mice. These data demonstrate that selective blockade of P2X7 receptors in vivo produces significant antinociception in animal models of inflammatory pain and suggest that the antihyperalgesic effects of P2X7 receptor blockade in an inflammatory pain model in mice are mediated by blocking the release of IL-1beta.

Recent patents on novel P2X(7) receptor antagonists and their potential for reducing central nervous system inflammation.[Pubmed:19705995]

Recent Pat CNS Drug Discov. 2010 Jan;5(1):35-45.

Inflammation arises in the CNS from a number of neurodegenerative and oncogenic disorders, as well as from ischemic and traumatic brain injuries. These pathologies give rise to increased levels of extracellular adenine nucleotides which, via activation of a variety of cell surface P2 purinergic receptors, influence the inflammatory activities of responding immune cells. One P2 receptor subtype in particular, the P2X(7) receptor, potentiates the release of pro-inflammatory cytokines, such as interleukin-1beta (IL-1beta) from macrophage-like cells. It is also thought to contribute to secondary brain injury by inducing neuronal cell death. Therefore, antagonism of this receptor could have significant therapeutic impact on all disorders, not just CNS, to which excessive inflammatory activities contribute. The use of currently available P2X(7) receptor antagonists for the treatment of CNS inflammation has been limited to the generally non-selective antagonists PPADS, oxidized ATP, Brilliant Blue G, suramin, calmidizolium, and KN-62. However, the recent patents and development of novel P2X(7) receptor antagonists, as discussed in this review, will provide new tools both for clinical and research purposes. Here we discuss compounds for which patents have been applied since 2006, from the following categories: benzamide inhibitors, bicycloheteroaryl compounds, acylhdranzine antagonists, biaromatic P2X(7) antagonists, heterocyclic compounds and amide derivatives, and aromatic amine antagonists.

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.

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