353791-85-2
Chemical Structure
J-113863
- CAS No.: 353791-85-2
- Formula:C30H37Cl2IN2O2
- Molecular Weight:655.44
IUPAC Name: (E)-1-(cyclooct-1-en-1-ylmethyl)-4-(2,7-dichloro-9H-xanthene-9-carboxamido)-1-ethylpiperidin-1-ium iodide
InChIKey: FOAFBMYSXIGAOX-LQGGPMKRSA-N
SMILES: CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(C3C4=C(OC5=C3C=C(Cl)C=C5)C=CC(Cl)=C4)=O)CC1.[I-]
Biological Activity: J-113863 is a potent and 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 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3].
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J-113863 | 95.19% | J-113863 is a potent and 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 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. | ||||||||||||||||||||
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J-113863 (Standard) | ≥98% | J-113863 (Standard) is the analytical standard of J-113863 (HY-103360). This product is intended for research and analytical applications. J-113863 is a potent and 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 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. | ||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
- [3]. Naya A, et al. Design, synthesis, and discovery of a novel CCR1 antagonist. J Med Chem. 2001 Apr 26;44(9):1429-35. [Content Brief]
