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PS372424 hydrochloride

Chemical Structure : PS372424 hydrochloride

CAS No.: 1596362-29-6

PS372424 hydrochloride (PS 372424 hydrochloride)

Catalog No.: PC-21815Not For Human Use, Lab Use Only.

PS372424 hydrochloride is a potent, selective peptidomimetic agonist of human CXC chemokine receptor 3 (CXCR3) with EC50 of 1.1 uM in calcium flux assays, binding affinity of 42 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PS372424 hydrochloride is a potent, selective peptidomimetic agonist of human CXC chemokine receptor 3 (CXCR3) with EC50 of 1.1 uM in calcium flux assays, binding affinity of 42 nM.
Unlike CXCL11, PS372424 does not stimulate transendothelial T-cell migration.
PS372424 is specific for human CXCR3 but does not activate murine CXCR3.
PS372424 activates ERK in T cells with a similar potency and kinetic to the natural ligand CXCL11.
PS372424 inhibits the migration of T cells toward CXCL11, CXCL12, and CCL5, whereas the CXCR3 antagonist NBI-74330 (Cat#PC-73268) only prevented migration toward CXCL11.
PS372424 demonstrates potent anti-inflammatory activity both in vitro and in a novel humanized in vivo model of rheumatoid arthritis.

Physicochemical Properties

M.Wt 625.21
Formula C33H45ClN6O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-((S)-1-((Cyclohexylmethyl)amino)-5-guanidino-1-oxopentan-2-yl)-2-(4-oxo-4-phenylbutanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide hydrochloride

References

1. Graeme O'Boyle, et al. Proc Natl Acad Sci U S A. 2012 Mar 20;109(12):4598-603.

2. Stroke IL, et al. Biochem Biophys Res Commun. 2006;349:221–228.

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