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    Immunology/Inflammation
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  3. J-113863

J-113863 

Cat. No.: HY-103360 Purity: >99.0%
Handling Instructions

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. 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.

For research use only. We do not sell to patients.

J-113863 Chemical Structure

J-113863 Chemical Structure

CAS No. : 353791-85-2

Size Price Stock
10 mM * 1  mL in DMSO USD 231 Ask For Quote & Lead Time
5 mg USD 160 Ask For Quote & Lead Time
10 mg USD 210 Ask For Quote & Lead Time
50 mg USD 680 Ask For Quote & Lead Time
100 mg USD 1050 Ask For Quote & Lead Time

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Description

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. 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].

IC50 & Target[2][3]

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.
Molecular Weight

655.44

Formula

C₃₀H₃₇Cl₂IN₂O₂

CAS No.

353791-85-2

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-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

J-113863J113863J 113863CCRCC chemokine receptorChemotaxisCCR1CCR3rheumatoidarthritisanti-inflammatorycollagenCD18Inhibitorinhibitorinhibit

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