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1627900-41-7

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1627900-41-7 Structure

1627900-41-7 Structure
IdentificationBack Directory
[Name]

(R)-(2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL)(1-(5-FLUOROPYRIDIN-2-YL)-4-METHYL-1,4,6,7-TETRAHYDRO-5H-IMIDAZO[4,5-C]PYRIDIN-5-YL)METHANONE
[CAS]

1627900-41-7
[Synonyms]

(R)-(2-CHLORO-3-(TRIFLUOROMETHYL)PHENYL)(1-(5-FLUOROPYRIDIN-2-YL)-4-METHYL-1,4,6,7-TETRAHYDRO-5H-IMIDAZO[4,5-C]PYRIDIN-5-YL)METHANONE
Methanone, [2-chloro-3-(trifluoromethyl)phenyl][(4R)-1-(5-fluoro-2-pyridinyl)-1,4,6,7-tetrahydro-4-methyl-5H-imidazo[4,5-c]pyridin-5-yl]-
[Molecular Formula]

C20H15ClF4N4O
[MDL Number]

MFCD30530737
[MOL File]

1627900-41-7.mol
[Molecular Weight]

438.81
Chemical PropertiesBack Directory
[Boiling point ]

586.7±50.0 °C(Predicted)
[density ]

1.49±0.1 g/cm3(Predicted)
[pka]

3.72±0.40(Predicted)
Hazard InformationBack Directory
[Uses]

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].
[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].

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).
[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 DOI:10.1021/acs.jmedchem.6b00989
1627900-41-7 suppliers list
Company Name: Jiangsu Nanchuang Chemical and Life Health Research Institute Co., Ltd.  
Telephone: 15720605021
Website: http://www.jsnchem.com/
Company Name: TargetMol Chemicals Inc.  
Telephone: 15002134094
Website: https://www.targetmol.cn/
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