JNJ-27141491

Research use only, not for human use.

A potent, selective, noncompetitive, orally active CCR2 antagonist with IC50 of 172 nM.

A potent, selective, noncompetitive, orally active CCR2 antagonist with IC50 of 172 nM; strongly suppresses MCP-1, -3, and -4-induced Ca(2+) mobilization; and leukocyte chemotaxis with IC50 of 7-97 nM, with no effect on other chemokine receptors; dose-dependently inhibits monocyte and neutrophil recruitment in mice.

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Animal Model:Transgenic mCCR2 knockout/hCCR2 knockin C57BL/6 mice Dosage:5, 10, 20, or 40 mg/kg Administration:Oral, once or twice daily Result:Once-daily oral treatment with 40, 20, 10, or 5 mg/kg inhibited the monocyte influx with 77, 57, 49, and 27%, respectively, compared with vehicle treatment, whereas this value was 74 and 22% after twice-daily oral treatment with 20 or 5 mg/kg. The neutrophil influx was also reduced; neutrophil numbers were decreased, with 56, 45, 20, and 8% after 40, 20, 10, or 5 mg/kg q.d. treatments and with 45 and 20% after 20 and 5 mg/kg b.i.d. treatments.

JNJ 27141491 | JNJ27141491

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

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871313-59-6

379.38

C17H15F2N3O3S

>98% (HPLC)

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O=C(C1=C(C2=CC=NO2)NC(N1[C@H](C3=CC=C(F)C(F)=C3)CC)=S)OC

3-[(1S)-1-(3,4-Difluorophenyl)propyl]-2,3-dihydro-5-(5-isoxazolyl)-2-thioxo-1H-imidazole-4-carboxylic acid methyl ester

(-20℃)

With Ice Pack

≥ 2 years