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MedChemExpressModel CXCR2-IN-1 -1873376-49-8

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CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC50 of 9.3.
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CXCR2-IN-1

MCE China:CXCR2-IN-1

Brand:MedChemExpress (MCE)

Cat. No.HY-101022

CAS:1873376-49-8

Purity:99.47%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description:CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC50 of 9.3.

In Vitro: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)[1].

In Vivo: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].

Animal Administration: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].

IC50 & Target:CXCR2 9.3 (pIC50)

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References:

[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.  [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
•   It has a professional experimental center and strict quality control and verification system;
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products;
•   The biological activity of the products has been verified by the experiments of customers in various countries;
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。