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CXCR2-IN-1
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。
CXCR2-IN-1图片
CAS NO:1873376-49-8
规格:≥98%
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 476.35
Formula C19H20Cl2FN3O4S
CAS No. 1873376-49-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>5 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES ClC1=CC=C(NC(NC2=CC=CC(F)=C2Cl)=O)C(O)=C1S(=O)(C3CCN(C)CC3)=O
Synonyms CXCR2-IN-1; CXCR2-IN 1; CXCR2 IN-1; CXCR2 IN 1
实验参考方法
In Vitro

In vitro activity: CXCR2-IN-1 is a novel CNs (central nervous system) penetrant antagonist of CXCR2 with a pIC50 of 9.3. It was discovered by structure-activity relationship exploration of the historical biarylurea series. CXCR2-IN-1 displayed nanomolar potency, favorable PK profile, and good developability potentials. More importantly, it showed efficacy in a cuprizone-induced demyelination model with twice daily oral administration, thereby supporting CXCR2 to be a potential therapeutic target for the treatment of demyelinating diseases such as multiple sclerosis.

Kinase Assay: CXCR2-IN-1 is a novel CNs (central nervous system) penetrant antagonist of CXCR2 with a pIC50 of 9.3. CXCR2 plays an important role in the activation and recruitment of neutrophils to sites of inflammation. CXCR2-IN-1 shows favorable central nervous system penetration property (Br/Bl>0.45)

Cell Assay:

In VivoCXCR2-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.
Animal model Mouse
Formulation & Dosage 30 and 100 mg/kg; p.o.
References