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JNJ-47965567

Catalog No. T4298   CAS 1428327-31-4
Synonyms: JNJ-479655

JNJ-47965567 (JNJ-479655) is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel(with pKis of 7.9 and 8.7 for human and rat P2X7, respectively).

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JNJ-47965567 Chemical Structure
JNJ-47965567, CAS 1428327-31-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 159.00
25 mg In stock $ 318.00
50 mg In stock $ 475.00
100 mg In stock $ 678.00
1 mL * 10 mM (in DMSO) In stock $ 87.00
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Purity: 99.76%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JNJ-47965567 (JNJ-479655) is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel(with pKis of 7.9 and 8.7 for human and rat P2X7, respectively).
Targets&IC50 P2X7 (human):7.9(pKis), P2X7 (rat):8.7(pKis)
In vitro JNJ-47965567 is potent high affinity (pKi 7.9 0.07), selective human P2X7 antagonist, with no significant observed speciation.?In native systems, the potency of the compound to attenuate IL-1β release was 6.7 0.07 (human blood), 7.5 0.07 (human monocytes) and 7.1 0.1 (rat microglia).?JNJ-47965567 exhibited target engagement in rat brain, with a brain EC50 of 78 19 ng·mL(-1) (P2X7 receptor autoradiography) and functional block of Bz-ATP induced IL-1β release.?JNJ-47965567 (30 mg·kg(-1) ) attenuated amphetamine-induced hyperactivity and exhibited modest, yet significant efficacy in the rat model of neuropathic pain.?No efficacy was observed in forced swim test.
Animal Research The authors used a combination of in vitro assays (calcium flux, radioligand binding, electrophysiology, IL-1β release) in both recombinant and native systems.?Target engagement of JNJ-47965567 was demonstrated by ex vivo receptor binding autoradiography and in vivo blockade of Bz-ATP induced IL-1β release in the rat brain.?Finally, the efficacy of JNJ-47965567 was tested in standard models of depression, mania and neuropathic pain
Synonyms JNJ-479655
Molecular Weight 488.64
Formula C28H32N4O2S
CAS No. 1428327-31-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 200 mg/mL (409.30 mM), Sonification is recommended.

TargetMolReferences and Literature

1. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567.[J]. British Journal of Pharmacology, 2013, 170(3):624-640.

TargetMolCitations

1. Chen J, Li T, Huang D, et al.Integrating UHPLC-MS/MS quantitative analysis and exogenous purine supplementation to elucidate the antidepressant mechanism of Chaigui granules by regulating purine metabolism.Journal of Pharmaceutical Analysis.2023

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Ion Channel Inhibitor Library Covalent Inhibitor Library

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Keywords

JNJ-47965567 1428327-31-4 Membrane transporter/Ion channel Neuroscience P2X Receptor Inhibitor P2X7 JNJ479655 JNJ 47965567 pain JNJ47965567 JNJ-479655 inhibit JNJ 479655 neuropathic P2XRs inhibitor

 

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