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Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C33H44N6O4 · 3H2O
CAS Number:
914291-61-5
Molecular Weight:
642.79
UNSPSC Code:
12352200
PubChem Substance ID:
12000484

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

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

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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