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JNJ-47965567
🥰Excellent
Catalog No. T4298Cas No. 1428327-31-4
Alias 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).
JNJ-47965567
🥰Excellent
Purity: 99.11%
Catalog No. T4298Alias JNJ-479655Cas No. 1428327-31-4
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).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $34 | In Stock | |
| 5 mg | $80 | In Stock | |
| 10 mg | $129 | In Stock | |
| 25 mg | $263 | In Stock | |
| 50 mg | $423 | In Stock | |
| 100 mg | $615 | In Stock | |
| 500 mg | $1,290 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $87 | In Stock |
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Purity:99.11%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 (rat):8.7(pKis), P2X7 (human):7.9(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 |
| Alias | JNJ-479655 |
| Molecular Weight | 488.64 |
| Formula | C28H32N4O2S |
| Cas No. | 1428327-31-4 |
| Smiles | O=C(NCC1(CCOCC1)N1CCN(CC1)c1ccccc1)c1cccnc1Sc1ccccc1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 200 mg/mL (409.30 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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