SX-517

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SX-517

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1240494-13-6

SX-517 是一种靶向CXCR2/1的双重拮抗剂，并且分子中含有硼酸。SX-517 还抑制 CXCL-1 诱导的 Ca²⁺通量 (IC₅₀=38 nM)，拮抗 CXCL-8 诱导的 [(35)S]GTPγS 结合作用 (IC₅₀=60 nM)，和ERK1/2磷酸化。SX-517 在人源多形核细胞 (PMN) 和小鼠模型中均具有显著的炎症抑制能力。

生物活性

SX-517 is a dualCXCR2/1antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca²⁺flux (IC₅₀=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC₅₀=60 nM) andERK1/2phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model^[1]^[2].

IC₅₀& Target^[1]

CXCR2

CXCR1

体外研究
(In Vitro)

SX-517 (compound 7) (0.1 nM-0.1 mM; 60 min) potently inhibits [35S]GTPγS binding induced by 10 nM CXCL8 with an IC50 of 60 nM^[1].
SX-517 (10 μM; 60 min) has inhibitory effect on the cell surface expression of CXCR2 in HEK293 cells^[1].
SX-517 (10 μM; 0-30 min) blocks CXCR2-mediated phosphorylation of ERK1/2 in HEK293 cells^[1].

Western Blot Analysis^[1]

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.

体内研究
(In Vivo)

SX-517 (compound 7) (0.2 mg/kg; iv; single dose) significantly inhibits inflammation in an in vivo murine model^[1].

Animal Model:	Male CD1 SWISS mice with an air-pouch on the backs (10-15 week old)^[1]
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.

分子量

382.22

Formula

C₁₉H₁₆BFN₂O₃S

CAS 号

1240494-13-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.