353791-85-2

中文名称 1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE

英文名称 1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE

CAS 353791-85-2

分子式 C30H37Cl2IN2O2

分子量 655.44

MOL 文件 353791-85-2.mol

更新日期 2024/10/07 18:47:54

353791-85-2 结构式

基本信息物理化学性质 1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE价格(试剂级) 常见问题列表

基本信息

中文别名

化合物J-113863

英文别名

J 113863
1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE

物理化学性质

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

常见问题列表

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。

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)

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.

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.