1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. JNJ-54166060

JNJ-54166060 

Cat. No.: HY-124300
Handling Instructions

JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively.

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

JNJ-54166060 Chemical Structure

JNJ-54166060 Chemical Structure

CAS No. : 1627900-41-7

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Description

JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptor, respectively[1].

IC50 & Target

IC50: 4/115/72 nM (human/rat/mouse P2X7 receptor)[1]

In Vivo

JNJ-54166060 exhibits high oral bioavailability (rat 55%, dog >100%, monkey 54 %) and Cmax (rat 375, dog 1249, monkey 389 ng/mL) following oral administration (rat 5 and, dog 5 mg/kg, monkey 5 mg/kg)[1].
JNJ-54166060 exhibits terminal elimination half-lives (rat 1.7 and, dog 11.9 h, monkey 4.2 h) due to low-moderate clearance (30, 5.5, and 14 mL/min/kg respectively) following intravenous administration (rat 1.0 and, dog 1.0 mg/kg, monkey 1.0 mg/kg)[1].

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

Animal Model: Sprague-Dawley rats[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (55%), Cmax (375 ng/mL), T1/2 (1.7 h).
Animal Model: Beagle dogs[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (>100%), Cmax (1249 ng/mL), T1/2 (11.9 h).
Animal Model: Cynomolgus monkeys[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (54%), Cmax (389 ng/mL), T1/2 (4.2 h).
Molecular Weight

438.81

Formula

C₂₀H₁₅ClF₄N₄O

CAS No.
SMILES

O=C(C1=CC=CC(C(F)(F)F)=C1Cl)N2CCC3=C(N=CN3C4=NC=C(F)C=C4)[[email protected]]2C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

JNJ-54166060JNJ54166060JNJ 54166060P2X ReceptorP2XRsP2X7ATPgatedpurinergicionchannelproinflammatorycytokinesInhibitorinhibitorinhibit

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