1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. JNJ-55308942

JNJ-55308942 

Cat. No.: HY-123857
Handling Instructions

JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.

For research use only. We do not sell to patients.

JNJ-55308942 Chemical Structure

JNJ-55308942 Chemical Structure

CAS No. : 2166558-11-6

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Description

JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain[1][2].

In Vitro

JNJ-55308942 shows pKis 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[2].

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[2].
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 ED50 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[2].
JNJ-55308942 (5 mg/kg; p.o.) shows the F, Vss, CL, Cmax and AUC24h values are 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sixteen male C57/BL6J mice[2]
Dosage: 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[1]
Dosage: P.o. (Pharmacokinetic Analysis)
Administration: 5 mg/kg
Result: The F, Vss, CL, Cmax and AUC24h were 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively.
Molecular Weight

425.32

Formula

C₁₇H₁₂F₅N₇O

CAS No.
SMILES

O=C(C1=C(F)C(C(F)(F)F)=NC=C1)N2[[email protected]@H](C)CC(N(C3=NC=C(F)C=N3)N=N4)=C4C2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

JNJ-55308942JNJ55308942JNJ 55308942P2X ReceptorP2XRsneuroinflammationanhedonianeuropsychopharmacologydepressionbrain-penetrantoralInhibitorinhibitorinhibit

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