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Cat. No.: HY-124300

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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.

CAS No.: 1627900-41-7
Formula: C₂₀H₁₅ClF₄N₄O
Molecular Weight:438.81

Storage:

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

Data Sheet (274 KB)

JNJ-54166060 Chemical Structure

CAS No.: 1627900-41-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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]

All P2X Receptor Isoforms :

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).

Chemical Information

CAS No. 1627900-41-7
Molecular Weight 438.81
Formula C₂₀H₁₅ClF₄N₄O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References

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JNJ-54166060

All P2X Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

JNJ-54166060 Related Classifications

HY-124300 Related Classifications