Chemical Structure : PS372424 hydrochloride
CAS No.: 1596362-29-6
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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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.
M.Wt | 625.21 | |
Formula | C33H45ClN6O4 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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 |
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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