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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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J655878-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $231.90 |
Specifications & Purity | 10mM in DMSO |
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Storage Temp | Protected from light,Desiccated,Store at -80°C |
Shipped In | Ice chest + Ice pads |
Product Description | JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC 50 =10 nM, K i =7.1 nM; rP2X7: IC 50 =15 nM, K i =2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain. In Vitro JNJ-55308942 shows pK i s of 8.1and 8.5 for recombinant human and rat P2X7 channels, respectively. In human blood and in mouse blood and microglia, JNJ-55308942 attenuates IL-1β release in a potent and concentration-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo JNJ-55308942 (30 mg/kg; p.o.) attenuates LPS-induced microglial activation in mice. In a model of Bacillus Calmette-Guerin (BCG)-induced depression, JNJ-55308942 dosed orally (30 mg/kg), reversed the BCG-induced deficits of sucrose preference and social interaction. After oral dosing, the compound exhibited both dose and concentration-dependent occupancy of rat brain P2X7 with an ED 50 of 0.07 mg/kg. The P2X7 antagonist (3 mg/kg, oral) blocked Bz-ATP-induced brain IL-1β release in conscious rats, demonstrating functional effects of target engagement in the brain. JNJ-55308942 (5 mg/kg; p.o.) shows the F, V ss , CL, C max and AUC 24h values are 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sixteen male C57/BL6J miceDosage: 30 mg/kg Administration: P.o. (after an i.p. injection of LPS (0.8 mg/kg, i.p.)) Result: Significantly attenuated the effect of LPS on FSC, CD45 surface expression and CD11b surface expression. Animal Model: Rat Dosage: P.o. (Pharmacokinetic Analysis) Administration: 5 mg/kg Result: The F, V ss , CL, C max and AUC 24h were 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively. |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Canonical SMILES | CC1CC2=C(CN1C(=O)C3=C(C(=NC=C3)C(F)(F)F)F)N=NN2C4=NC=C(C=N4)F |
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Molecular Weight | 425.32 |
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