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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $70 | In Stock | |
5 mg | $172 | In Stock | |
10 mg | $278 | In Stock | |
25 mg | $537 | In Stock | |
50 mg | $775 | In Stock | |
100 mg | $1,080 | In Stock | |
500 mg | $2,170 | In Stock | |
1 mL x 10 mM (in DMSO) | $189 | In Stock |
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]. |
Molecular Weight | 425.32 |
Formula | C17H12F5N7O |
Cas No. | 2166558-11-6 |
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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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