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

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

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
中文同义词化合物J-113863;1-(1-环辛烯-1-基甲基)-4-[[(2,7-二氯-9H-氧杂蒽-9-基)羰基]氨基]-1-乙基哌啶鎓碘化物
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
英文同义词1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE;J 113863;CCR,Inhibitor,inhibit,rheumatoid,J-113863,CCR1,CCR3,CC chemokine receptor,Chemotaxis,collagen,arthritis,J 113863,J113863,CD18,anti-inflammatory
CAS号353791-85-2
分子式C30H37Cl2IN2O2
分子量655.44
EINECS号
相关类别
Mol文件353791-85-2.mol
结构式1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE 结构式

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

储存条件Store at +4°C
溶解度在 DMSO 中溶解度为 100 mM,在乙醇中溶解度为 50 mM
形态粉末
颜色浅黄至黄色

1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE 用途与合成方法

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。

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)

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.

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-103360J-1138631 mg727元
2024/04/30HY-1033601,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE
J-113863
353791-85-25mg1600元

1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE 上下游产品信息

"1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE"相关产品信息
吨-9-碳乙酰胺
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