1873376-49-8

1873376-49-8 structure

Name: CXCR2-IN-1
Chemical Name: CXCR2-IN-1
CAS Number: 1873376-49-8
Molecular Formula: C₁₉H₂₀Cl₂FN₃O₄S
Molecular Weight: 476.349
Catalog: Research Areas Inflammation/Immunology
Create Date: 2018-06-29 01:41:12
Modify Date: 2024-01-31 22:33:03
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.

Name	CXCR2-IN-1
Synonyms	1-(2-Chloro-3-fluorophenyl)-3-{4-chloro-2-hydroxy-3-[(1-methyl-4-piperidinyl)sulfonyl]phenyl}urea Urea, N-(2-chloro-3-fluorophenyl)-N'-[4-chloro-2-hydroxy-3-[(1-methyl-4-piperidinyl)sulfonyl]phenyl]-

Description	CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
Related Catalog	Research Areas >> Inflammation/Immunology
Target	CXCR2:9.3 (pIC50)
In Vitro	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].
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 Admin	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].
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.