1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. J-113863

J-113863 

Cat. No.: HY-103360
Handling Instructions

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 has no active 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 Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All CCR Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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 has no active 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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

J-113863J113863J 113863CCRCC chemokine receptorChemotaxisCCR1CCR3rheumatoidarthritisanti-inflammatorycollagenInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
J-113863
Cat. No.:
HY-103360
Quantity:
MCE Japan Authorized Agent: