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353791-85-2

中文名稱 1,4-CIS-1-(1-CYCLOOCTEN-1-YLMETHYL)-4-[[(2,7-DICHLORO-9H-XANTHEN-9-YL)CARBONYL]AMINO]-1-ETHYLPIPERIDINIUM IODIDE
英文名稱 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 2024/12/15 19:35:18
353791-85-2 結(jié)構(gòu)式 353791-85-2 結(jié)構(gòu)式

基本信息

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

物理化學(xué)性質(zhì)

儲存條件Store at +4°C
溶解度Soluble to 100 mM in DMSO and to 50 mM in ethanol
形態(tài)Powder
顏色Light yellow to yellow

常見問題列表

生物活性
J-113863 是一種有效的選擇性的 CCR1 (CD18) 拮抗劑,對人和小鼠 CCR1 受體的 IC50 值分別為 0.9 nM 和 5.8 nM。J-113863 是人 CCR3 的強效拮抗劑 (IC50 為 0.58 nM),還是小鼠 CCR3 的弱效拮抗劑 (IC50 為 460 nM)。J-113863 對 CCR2,CCR4 和 CCR5 以及 LTB4 或 TNF-α 受體沒有活性??寡鬃饔?。
靶點

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)

體外研究

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.

體內(nèi)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.
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