CXCR2-IN-1

Names

[ Name ]:
CXCR2-IN-1

[Synonym ]:
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]-

Biological Activity

[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.

[Related Small Molecules]

Reparixin | AMG 487 | SCH 527123 | SB 225002 | AZD-5069 | LY2510924 | SCH 546738 | TAK-779 | BKT140 acetate salt | Danirixin | AZD8797 | Baohuoside I | SCH 563705 | IT1t dihydrochloride

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
538.1±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₂₀Cl₂FN₃O₄S

[ Molecular Weight ]:
476.349

[ Flash Point ]:
279.2±30.1 °C

[ Exact Mass ]:
475.053558

[ LogP ]:
4.64

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.647

[ Storage condition ]:
2-8℃

Related Compounds

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