239823

CXCR3 Agonist, PS372424

The CXCR3 Agonist, PS372424 controls the biological activity of CXCR3. This small molecule/inhibitor is primarily used for Cell Signaling applications.

• Synonym(s): CXCR3 Agonist, PS372424, (S)-N-((S)-1-((cyclohexylmethyl)amino)-5-guanidino-1-oxopentan-2-yl)-2-(4-oxo-4-phenylbutanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, Chemokine (C-X-C motif) Receptor 3 Agonist
• Empirical Formula (Hill Notation): C₃₃H₄₄N₆O₄ · 3H₂O
• CAS Number: 914291-61-5
• Molecular Weight: 642.79
• UNSPSC Code: 12352200
• PubChem Substance ID: 12000484

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C
• SMILES string: C1CCC(CC1)CNC(=O)C(CCCN=C(N)N)NC(=O)C2CC3=CC=CC=C3CN2C(=O)CCC(=O)C4=CC=CC=C4

Description

General description

A peptidomimetic derivative containing tetrahydroisoquinoline-arginine motif that aligns with a Pro-Arg motif of CXCL10. Acts as a highly specific agonist of human CXCR3 (EC₅₀ = 1.1 mM, competitive CXCL10 binding IC₅₀ = 42 nM). Does not affect murine CXCR3. Induces a long-lasting internalization of about 87% of cell-surface CXCR3 within 30 min. Effectively stimulates T-cell migration (~ 50 nM) and blocks the migration of activated T cells towards CXCL11, CXCL12, and CCL5. Also reduces the migration of activated T cells towards rheumatoid arthritis synovial fibroblasts (RASF). Shown to induce phosphorylation of ERK with similar potency and kinetics as CXCL11. Also shown to block CXCL11 induced migration of CD45+ cells to air pouches generated on humanized mice.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

O′Boyle, G., et al. 2012, PNAS.109, 4598.
Stroke, I. L., et al. 2006, Biochem Biophys Res Comm.349, 221.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable