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J-113863

Catalog No. T11699 CAS 353791-85-2

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. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

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J-113863, CAS 353791-85-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 79.00
5 mg	In stock	$ 128.00
10 mg	In stock	$ 172.00
25 mg	In stock	$ 319.00
50 mg	In stock	$ 555.00
100 mg	In stock	$ 798.00
1 mL * 10 mM (in DMSO)	In stock	$ 189.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	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. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.
Targets&IC50	CCR3:0.58 nM (IC50, Human CCR3), CCR3:460 nM (IC50, Mouse CCR3), CCR1:0.9 nM (IC50, Human CCR1), CCR1:5.8 nM (IC50, Mouse CCR1)
In vitro	The chemotaxis of the following cells were inhibited by J-113863. 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.
In vivo	J-113863 treatment improves paw inflammation and joint damage, and dramatically decreases cell infiltration into joints in arthritic mice.

Molecular Weight	655.44
Formula	C30H37Cl2IN2O2
CAS No.	353791-85-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6.56 mg/mL (10 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Bioactive Compound Library Immuno-Oncology Compound Library Cytokine Inhibitor Library Anti-Aging Compound Library NO PAINS Compound Library Anti-Fibrosis Compound Library Chemokine Inhibitor Library

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Keywords

J-113863 353791-85-2 Immunology/Inflammation Microbiology/Virology CCR Inhibitor inhibit rheumatoid CCR1 CCR3 J 113863 CC chemokine receptor Chemotaxis collagen arthritis J113863 CD18 anti-inflammatory inhibitor

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