JNJ-54166060

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

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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]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 10 μM Compound: 1; JNJ 54166060	Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by competitive binding assay Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by competitive binding assay	[PMID: 27548392]

In Vivo

JNJ-54166060 exhibits high oral bioavailability (rat 55%, dog >100%, monkey 54 %) and C_max (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%), C_max (375 ng/mL), T_1/2 (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%), C_max (1249 ng/mL), T_1/2 (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%), C_max (389 ng/mL), T_1/2 (4.2 h).

Molecular Weight

438.81

Formula

C₂₀H₁₅ClF₄N₄O

CAS No.

1627900-41-7

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

Handling Instructions (2659 KB)

References

[1]. Devin M Swanson, et al. Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. J Med Chem. 2016 [Content Brief]

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.

Keywords:

JNJ-541660601627900-41-7JNJ54166060JNJ 54166060P2X ReceptorP2XRsP2X7ATPgatedpurinergicionchannelproinflammatorycytokinesInhibitorinhibitorinhibit

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