CXCR2-IN-1

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

一种有效的 CNS 渗透性 CXCR2 拮抗剂，pIC50 为 9.3；显示中性粒细胞趋化性抑制，pIC50 为 7.6。

A potent, CNS penetrant CXCR2 antagonist with pIC50 of 9.3; shows neutrophil chemotaxis inhibition with pIC50 of 7.6; has developability profiles (CYP inhibition pIC<5.0, and hERG binding affinity pIC<4.0); exhibits favorable PK profile, reasonable CNS penetration, and good developability potential; orally bioavailable.

CXCR2 plays an important role in the activation and recruitment of neutrophils to sites of inflammation. CXCR2-IN-1 (compound 22) shows favorable central nervous system penetration property (Br/Bl>0.45).

CXCR2-IN-1 shows efficacy in a cuprizone-induced demyelination model through oral administration, providing evidence to support CXCR2 to be a potential therapeutic target to treat demyelinating diseases such as multiple sclerosis.

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GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

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1873376-49-8

476.3492032

C19H20Cl2FN3O4S

>98% (HPLC)

DMSO: ≥5.4 mg/mL (Need ultrasonic and warming)

CN1CCC(CC1)S(=O)(=O)C2=C(C=CC(=C2O)NC(=O)NC3=C(C(=CC=C3)F)Cl)Cl

Urea, N-(2-chloro-3-fluorophenyl)-N'-[4-chloro-2-hydroxy-3-[(1-methyl-4-piperidinyl)sulfonyl]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years