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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-PS372424
PS372424

Chemical Structure : PS372424

CAS No.: 914291-61-5

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PS372424 (PS 372424)

货号: PC-21814Not For Human Use, Lab Use Only.

PS372424 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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5 mg ￥2280 In stock
10 mg ￥3680 In stock
25 mg ￥5880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PS372424 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.

物理化学性质&存储条件

分子量 588.75
分子式 C33H44N6O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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