J 113863
Modify Date: 2024-01-08 05:42:36
J 113863 structure
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Common Name | J 113863 | ||
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| CAS Number | 353791-85-2 | Molecular Weight | 655.43700 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C30H37Cl2IN2O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of J 113863J-113863 is a potentand selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 has no active against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3]. |
| Name | 2,7-dichloro-N-[1-(cycloocten-1-ylmethyl)-1-ethylpiperidin-1-ium-4-yl]-9H-xanthene-9-carboxamide,iodide |
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| Synonym | More Synonyms |
| Description | J-113863 is a potentand selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 has no active against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3]. |
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| Related Catalog | |
| Target |
CCR1:0.9 nM (IC50, Human CCR1) CCR1:5.8 nM (IC50, Mouse CCR1) CCR3:0.58 nM (IC50, Human CCR3) CCR3:460 nM (IC50, Mouse CCR3) |
| In Vitro | 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[1]. |
| In Vivo | 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[2]. Animal Model: DBA-1 male mice (10-12 weeks) induced with Collagen[2] 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. |
| References |
| Molecular Formula | C30H37Cl2IN2O2 |
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| Molecular Weight | 655.43700 |
| Exact Mass | 654.12800 |
| PSA | 38.33000 |
| LogP | 4.98060 |
| Piperidinium, 1-[(1E)-1-cycloocten-1-ylmethyl]-4-[[(2,7-dichloro-9H-xanthen-9-yl)carbonyl]amino]-1-ethyl-, iodide (1:1) |
| 1-[(1E)-1-Cycloocten-1-ylmethyl]-4-{[(2,7-dichloro-9H-xanthen-9-yl)carbonyl]amino}-1-ethylpiperidinium iodide |