JNJ-27141491 ( JNJ 27141491 | JNJ27141491 )

产品货号. M16331 CAS No. 871313-59-6

COA

Datasheet

HNMR

HPLC

MSDS

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产品名称

JNJ-27141491
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

一种有效的、选择性的、非竞争性的、口服活性的 CCR2 拮抗剂，IC50 为 172 nM。
产品描述

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.
体外实验

——
体内实验

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.
同义词

JNJ 27141491 | JNJ27141491
通路

GPCR/G Protein
靶点

Chemokine Receptor
受体

Chemokine Receptor
研究领域

——
适应症

——

CAS Number

871313-59-6
分子量

379.38
分子式

C17H15F2N3O3S
纯度

>98% (HPLC)
溶解度

——
SMILES

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

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

1. Zweemer AJ, et al. Mol Pharmacol. 2013 Oct;84(4):551-61. 2. Buntinx M, et al. J Pharmacol Exp Ther. 2008 Oct;327(1):1-9.

计算器

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