2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. JNJ-27141491

JNJ-27141491 是一种选择性、非竞争性和具有口服活性的人 CCR2 的功能性拮抗剂。

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JNJ-27141491 Chemical Structure

JNJ-27141491 Chemical Structure

CAS No. : 871313-59-6

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JNJ-27141491 相关抗体

Top Publications Citing Use of Products

查看 CCR 亚型特异性产品:

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target[1]

hCCR2

 

体外研究
(In Vitro)

JNJ-27141491 抑制 MCP-1 诱导的 [35S]GTPγS 与 hCCR2-CHO 细胞膜的结合 (IC50=38±9 nM)，并减少 MCP-1 诱导的 Ca2+ 动员，在 hCCR2-CHO 细胞的 IC50 为 13±1 nM，在 THP-1 细胞的 IC50 为 13±2 nM 和在人血单核细胞的 IC50 为 43±4 nM。JNJ-27141491 也抑制人 PBMC 对 MCP-1 的趋化作用，其 IC50 值为 97±16 nM[1]。
JNJ-27141491 与 MCP-1 和 hCCR2 的结合竞争，并作为 CCR2 受体的非竞争性拮抗剂[1]。

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

JNJ-27141491 相关抗体:
体内研究
(In Vivo)

JNJ-27141491 (5-40 mg/kg; oral; once or twice daily) 抑制单核细胞和中性粒细胞招募到转基因 hCCR2 敲入小鼠的肺泡空气空间[1]。
JNJ-27141491 (20 mg/kg; oral; daily for 16 days) 在转基因 CCR2 小鼠中延迟实验性自身免疫性脑脊髓炎 (EAE)[1]。

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.
分子量

379.38

Formula

C17H15F2N3O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

JNJ-27141491 相关分类

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  • 稀释计算器

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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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产品名称：
JNJ-27141491
目录号：
HY-110132
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