JNJ-27141491

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JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2.

For research use only. We do not sell to patients.

JNJ-27141491 Chemical Structure

CAS No. : 871313-59-6

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Description

JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2^[1].

IC₅₀ & Target^[1]

hCCR2

In Vitro

JNJ-27141491 inhibits MCP-1-induced [³⁵S]GTPγS binding to hCCR2-CHO cell membranes (IC₅₀=38±9 nM) and reduces MCP-1-induced Ca²⁺ mobilization in hCCR2-CHO cells (IC₅₀=13±1 nM), in THP-1 cells (IC₅₀=13±2 nM), and in human blood monocytes (IC₅₀=43±4 nM). JNJ-27141491 also inhibits chemotaxis of human PBMC toward MCP-1, with an IC₅₀ value of 97±16 nM^[1].
JNJ-27141491 competes with the binding of MCP-1 to hCCR2 and acts as a noncompetitive antagonist of the CCR2 receptor^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JNJ-27141491 (5-40 mg/kg; oral; once or twice daily) inhibits recruitment of monocytes and neutrophils into the alveolar air space of transgenic hCCR2 knockin mice^[1].
JNJ-27141491 (20 mg/kg; oral; daily for 16 days) delays experimental autoimmune encephalomyelitis (EAE) in transgenic CCR2 mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Transgenic mCCR2 knockout/hCCR2 knockin C57BL/6 mice^[1]
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.

Molecular Weight

379.38

Formula

C₁₇H₁₅F₂N₃O₃S

CAS No.

871313-59-6

SMILES

CC[C@@H](C1=CC(F)=C(F)C=C1)N2C(C(OC)=O)=C(C3=CC=NO3)NC2=S

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]. Buntinx M, et al. Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor CCR2. J Pharmacol Exp Ther. 2008 Oct;327(1):1-9. [Content Brief]

JNJ-27141491 Related Classifications

Inflammation/Immunology

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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-27141491871313-59-6JNJ27141491JNJ 27141491CCRCC chemokine receptororally activeMCP-1CHOmonocytesneutrophilsexperimental autoimmune encephalomyelitisInhibitorinhibitorinhibit

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