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

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].

MedChemExpress (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)[C@H]2C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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JNJ-54166060 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
JNJ-54166060
Cat. No.:
HY-124300
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