CXCR2-IN-68

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

CXCR2-IN-68 是一种有效、选择性、脑渗透性、口服生物可利用的 CXCR2 拮抗剂，pIC50 为 9.0。

CXCR2-IN-68 is a potent, selective, brain penetrant, and orally bioavailable CXCR2 antagonist with pIC50 of 9.0, displays 730-fold selectivity over CXCR1 and >1,900-fold selectivity over all other chemokine receptors; inhibits human whole blood Gro-α induced CD11b expression with IC50 of 0.04 μM, 17-fold more potent than Navarixin; significantly inhibits neutrophil infiltration in mouse at 1, 3, 10 mg/kg oral dosing twice daily (BID).

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CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models. Animal Model:6-8 week old male C57Bl/6 mice (Air Pouch Model in Mouse)Dosage:1, 3, and 10 mg/kg Administration:P.o.; twice daily for 3 days Result:Significantly inhibited neutrophil infiltration into mouse air pouch.Animal Model:8-10 week old male Wistar rats (Air Pouch Model in Rat)Dosage:1, 3, and 10 mg/kg Administration:P.o.; twice daily for 3 days Result:Inhibited neutrophil migration to air pouch in rat.

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GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

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1838123-21-9

414.901

C18H23ClN2O5S

>98% (HPLC)

In Vitro:?DMSO : 240 mg/mL (578.45 mM)

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1-(4-chloro-2-hydroxy-3-(((S)-3-methyltetrahydrofuran-3-yl)sulfonyl)phenyl)-3-((R)-2-methylcyclopent-2-en-1-yl)urea

(-20℃)

With Ice Pack

≥ 2 years