Top Suppliers:I want be here
Related CAS#:
202796-41-6 202796-42-7
353791-85-2 198279-45-7
1146963-51-0 71712-05-5
2387505-73-7 854812-04-7
715-99-1 187937-24-2

353791-85-2

353791-85-2 structure
353791-85-2 structure
  • Name: J 113863
  • Chemical Name: 2,7-dichloro-N-[1-(cycloocten-1-ylmethyl)-1-ethylpiperidin-1-ium-4-yl]-9H-xanthene-9-carboxamide,iodide
  • CAS Number: 353791-85-2
  • Molecular Formula: C30H37Cl2IN2O2
  • Molecular Weight: 655.43700
  • Catalog: Signaling Pathways GPCR/G Protein CCR
  • Create Date: 2016-08-04 04:54:25
  • Modify Date: 2024-01-08 05:42:36
  • 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].
Name 2,7-dichloro-N-[1-(cycloocten-1-ylmethyl)-1-ethylpiperidin-1-ium-4-yl]-9H-xanthene-9-carboxamide,iodide
Synonyms 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
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].
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

[1]. Lehmann MH, et al. Modified Vaccinia virus Ankara but not vaccinia virus induces chemokine expression in cells of the monocyte/macrophage lineage. Virol J. 2015 Feb 12;12:21.

[2]. Amat M, et al. Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo. Br J Pharmacol. 2006 Nov;149(6):666-75.

[3]. Naya A, et al. Design, synthesis, and discovery of a novel CCR1 antagonist. J Med Chem. 2001 Apr 26;44(9):1429-35.
Molecular Formula C30H37Cl2IN2O2
Molecular Weight 655.43700
Exact Mass 654.12800
PSA 38.33000
LogP 4.98060

Chemsrc provides CAS#:353791-85-2 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 353791-85-2 | Chemsrc address: https://m.chemsrc.com/en/baike/600019.html

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved