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J-113863

SKU: orb1309532

Description

J-113863 is a potent and selective CCR1 antagonist with species-specific activity, showing high affinity for human CCR1 (IC50 0.9 nM) and mouse CCR1 (IC50 5.8 nM). It also antagonizes human CCR3 but is much less active on the mouse ortholog, and is inactive against several other chemokine and inflammatory receptors. This profile makes it a valuable research tool for studying CCR1-mediated pathways in inflammation, autoimmunity, and fibrosis in both cellular and animal models.

Research Area

Immunology & Inflammation, Infectious Disease & Virology, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number353791-85-2
MW655.44
Purity95.11% (May vary between batches)
FormulaC30H37Cl2IN2O2
SMILES[I-].CC[N+]1(C\C2=C\CCCCCC2)CCC(CC1)NC(=O)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc12
TargetCCR
SolubilityDMSO:6.56 mg/mL (10.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.53 mM)

Bioactivity

Target 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 Vivo
J-113863 treatment improves paw inflammation and joint damage, and dramatically decreases cell infiltration into joints in arthritic mice.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

collagen, CCR1, CCR, CC chemokine receptor, CCR3, Chemotaxis, CD18, arthritis, anti-inflammatory, Inhibitor, inhibit, J 113863, J113863, J-113863, rheumatoid

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  • J-113863 [orb1219516]

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Key Properties

No computed properties available.

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Protocol Information

J-113863 (orb1309532)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 100.00
2 mg
$ 120.00
5 mg
$ 170.00
10 mg
$ 220.00
1 ml x 10 mM (in DMSO)
$ 230.00
25 mg
$ 360.00
50 mg
$ 600.00
100 mg
$ 840.00
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