Name | JNJ-55308942 |
Description | JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively. |
In vitro | JNJ-55308942 shows pKis of 8.1and 8.5 for recombinant hP2X7 and rP2X7. JNJ-55308942 attenuates IL-1β release in a concentration-dependent manner in human blood and in mouse blood and microglia[2]. |
In vivo | JNJ-55308942 (5 mg/kg; p.o.) shows the F of 81%, Vss of 1.7 L/kg, CL of 1.7 L/kg, Cmax of 3.7 mL min/kg, and AUC of 1747 ng/mL[1]. In male C57/BL6J mice, JNJ-55308942 (30 mg/kg; p.o.) significantly attenuates the effect of LPS on FSC, CD45 surface expression, and CD11b surface expression. In a model of Bacillus Calmette-Guerin-induced depression, JNJ-55308942 (30 mg/kg; orally) reverses the BCG-induced deficits of sucrose preference and social interaction (ED50 = 0.07 mg/kg). The P2X7 antagonist (3 mg/kg, orally) blocks Bz-ATP-induced brain IL-1β release in conscious rats[2]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 90 mg/mL (211.6 mM), Sonication is recommended.
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Keywords | JNJ 55308942 | JNJ-55308942 | JNJ55308942 |
Inhibitors Related | Opiranserin hydrochloride | Aurintricarboxylic acid | (E/Z)-Sivopixant | PSB-12062 | ATP disodium salt | Oxatomide | JNJ-42253432 | Ivermectin | Lappaconitine | CTP disodium dihydrate | AF-353 | Brilliant blue G-250 |
Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library |