1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE
- CAS号:353791-85-2
- 英文名:1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE
- 中文名:1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE
- CBNumber:CB72453425
- 分子式:C30H37Cl2IN2O2
- 分子量:655.44
- MOL File:353791-85-2.mol
- 储存条件 :Store at +4°C
- 溶解度 :Soluble to 100 mM in DMSO and to 50 mM in ethanol
- 形态 :Powder
- 颜色 :Light yellow to yellow
1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE性质、用途与生产工艺
- 生物活性 J-113863 是一种有效的选择性的 CCR1 (CD18) 拮抗剂,对人和小鼠 CCR1 受体的 IC50 值分别为 0.9 nM 和 5.8 nM。J-113863 是人 CCR3 的强效拮抗剂 (IC50 为 0.58 nM),还是小鼠 CCR3 的弱效拮抗剂 (IC50 为 460 nM)。J-113863 对 CCR2,CCR4 和 CCR5 以及 LTB4 或 TNF-α 受体没有活性。抗炎作用。
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靶点
CCR1
0.9 nM (IC 50 , Human CCR1)
CCR1
5.8 nM (IC 50 , Mouse CCR1)
CCR3
0.58 nM (IC 50 , Human CCR3)
CCR3
460 nM (IC 50 , Mouse CCR3)
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体外研究
Modified Vaccinia virus Ankara (MVA) but not MVA and vaccinia virus (VACV) infected MH-S cells increase the expression of the CXCR2 acting chemokine CXCL2. MH-S cells constitutively produce CCL2 and CCR1 acting chemokines CCL3, CCL5 and CCL9. Consequently, supernatants of mock treated and virus infected MH-S cells induce chemotaxis of murine promyelocyte MPRO cells and human monocytic THP-1 cells at the same level. However, supernatants of MVA infected MH-S cells significantly increase chemotaxis of the CCR2 deficient human monocytic cell line U-937. Chemotaxis of all above cell types is inhibited by J-113863.
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体内研究
J-113863 (3-10 mg/kg; intraperitoneal injection; once daily; for 11 days; DBA-1 male mice) treatment improves paw inflammation and joint damage, and dramatically decreases cell infiltration into joints in arthritic mice.
Animal Model: DBA-1 male mice (10-12 weeks) induced with Collagen Dosage: 3 mg/kg, 10 mg/kg Administration: Intraperitoneal injection; once daily; for 11 days Result: Improved paw inflammation and joint damage, and dramatically decreased cell infiltration into joints.
- 更新日期:2024/11/08
- 产品编号:HY-103360
- 产品名称:J-113863
- CAS编号:
- 包装:1 mg
- 价格:727元
- 更新日期:2024/11/08
- 产品编号:HY-103360
- 产品名称:1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE J-113863
- CAS编号:353791-85-2
- 包装:5mg
- 价格:1600元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5726
- 优势度:77