CXCR2-IN-1

CXCR2-IN-1是可渗透中枢神经系统的CXCR2拮抗剂，pIC50值为9.3。

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库存: 现货

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1mg

￥1612.00

1290.00

- +
5mg

￥3737.00

2990.00

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10mg

￥6412.00

5130.00

- +
25mg

￥12712.00

10170.00

- +
50mg

￥20662.00

16530.00

- +
100mg

￥36025.00

28820.00

- +

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Background

CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists 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)[1].

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[1].

[1]. Xu H, et al. Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders. ACS Med Chem Lett. 2016 Feb 8;7(4):397-402.

Protocol

Animal experiment:

Mice: Mice are fed with cuprizone for 5 weeks to cause demyelinating lesions in the CNS and then orally administrated with CXCR2-IN-1 for 9 consecutive days at doses of 30 and 100 mg/kg twice daily[1].

参考文献:

[1]. Xu H, et al. Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders. ACS Med Chem Lett. 2016 Feb 8;7(4):397-402.