| 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 | |
| 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 |
| 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℃ |