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DF2755A

Chemical Structure : DF2755A

CAS No.: 1218784-94-1

DF2755A (DF-2755A)

Catalog No.: PC-38704Not For Human Use, Lab Use Only.

DF2755A is a selective, allosteric, orally acting inhibitor of CXCR1/2 (Kd=2.24/0.94 nM), inhibits human PMN (hPMN) migration induced by CXCL8 and CXCL1 with IC50 of 4.2 and 2.1 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DF2755A is a selective, allosteric, orally acting inhibitor of CXCR1/2 (Kd=2.24/0.94 nM), inhibits human PMN (hPMN) migration induced by CXCL8 and CXCL1 with IC50 of 4.2 and 2.1 nM, respectively.
DF2755A is equally efficacious in inhibiting CXCL8- and CXCL1-induced hPMN chemotaxis induced by an optimal concentration of CXCL8 (1 nM) or CXCL1 (10 nM).
DF2755A selectively inhibited neutrophil chemotaxis induced by CXCR1/2 ligands without effect on CXCL8 binding to neutrophils.
DF2755A (3-30 mg/kg, p.o.) reduced inflammatory hyperalgesia induced by carrageenan, LPS and CXCL1/KC as well as neutrophil recruitment and IL-1β production in vivo.

Physicochemical Properties

M.Wt 338.280
Formula C13H10F3N2NaO2S
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

sodium (2S)-2-(4-{[4-(trifluoromethyl)-1,3-thiazol-2-yl]amino}phenyl) propanoate

References

1. Lopes AH,, et al. Pharmacol Res. 2016 Jan;103:69-79.

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