871313-59-6
871313-59-6 structure
- Name: JNJ-27141491
- Chemical Name: Methyl 3-[(1S)-1-(3,4-difluorophenyl)propyl]-5-(1,2-oxazol-5-yl)-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxylate
- CAS Number: 871313-59-6
- Molecular Formula: C17H15F2N3O3S
- Molecular Weight: 379.381
- Catalog: Signaling Pathways GPCR/G Protein CCR
- Create Date: 2018-06-02 08:06:55
- Modify Date: 2024-02-15 18:29:34
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JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2[1].
| Name | Methyl 3-[(1S)-1-(3,4-difluorophenyl)propyl]-5-(1,2-oxazol-5-yl)-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxylate |
|---|---|
| Synonyms |
1H-Imidazole-4-carboxylic acid, 3-[(1S)-1-(3,4-difluorophenyl)propyl]-2,3-dihydro-5-(5-isoxazolyl)-2-thioxo-, methyl ester
Methyl 3-[(1S)-1-(3,4-difluorophenyl)propyl]-5-(1,2-oxazol-5-yl)-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxylate JNJ-27141491 |
| Description | JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2[1]. |
|---|---|
| Related Catalog | |
| Target |
hCCR2 |
| 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]。 |
| 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]。 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. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 501.8±60.0 °C at 760 mmHg |
| Molecular Formula | C17H15F2N3O3S |
| Molecular Weight | 379.381 |
| Flash Point | 257.3±32.9 °C |
| Exact Mass | 379.080231 |
| LogP | 2.10 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Index of Refraction | 1.626 |