SX-517

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、特异性、非竞争性双重 CXCR1 和 CXCR2 拮抗剂，IC50 分别为 38 nM（相对于 CXCL1）和 36 nM（相对于 CXCL8）。

A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively; inhibits CXCL1-induced Ca(2+) flux in human PMNs but has no effect on the Ca(2+) flux induced by C5a, fMLF, or PAF; antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation in recombinant HEK293 cells expressed CXCR2; significantly inhibits inflammation in an in vivo murine model (0.2 mg/kg iv).

Western Blot Analysis Cell Line:HEK293 cells Concentration:10 μM; with or without 100 ng/mL CXCL-8 Incubation Time:0, 5, 15, 30 min Result:Completely blocked CXCL-8-induced phosphorylation of ERK1/2 by 30 min.

Animal Model:Male CD1 SWISS mice with an air-pouch on the backs (10-15 week old)Dosage:0.02 mg/kg, 0.2 mg/kg Administration:Intravenous injection; single dose Result:Significant reduction in cell count in the pouches of treated animals compared to the positive control cohort.

Phenylboronic Acid | SX 517 | SX517

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

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1240494-13-6

382.216

C19H16BFN2O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (261.63 mM)

OB(C1=CC=CC=C1CSC2=NC=C(C(NC3=CC=C(F)C=C3)=O)C=C2)O

2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid

(-20℃)

With Ice Pack

≥ 2 years