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SB 332235
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C13H10Cl3N3O4S
- MW: 410.66
Description
SB 332235 is a potent and selective nonpeptide CXCR2 antagonist with IC50 values of 9.3 nM and 9.6 µM for CXCR2 and CXCR1, respectively. It exhibits significant anti-inflammatory effects in acute and chronic models of arthritis in the rabbit. SB-332235 significantly reduced levels of proinflammatory mediators in the synovial fluid, including TNF-α, IL-8, PGE2, LTB4, and LTC4.
CXCR2 pharmacology is relevant to arthritis; SB 332235 supports mechanistic studies of CXCR2, TNF-α, IL-8 in biochemical, cellular and disease-model assays.
Key Features
- Potent and selective CXCR2 antagonist
- IC50: 9.3 nM for CXCR2 and 9.6 µM for CXCR1
- Modulates CXCR2-dependent signaling or biological activity
- Supports focused CXCR2 pathway studies in biochemical and cellular systems
Applications
- CXCR2 pharmacology and target-validation studies
- CXCR2 pathway and signaling assays
- Disease-model research related to arthritis
- Receptor signaling, ligand profiling and functional response assays
More Information
| Parent CAS No. | 276702-15-9 |
|---|---|
| Chemical Name | 6-chloro-3-(3-(2,3-dichlorophenyl)ureido)-2-hydroxybenzenesulfonamide |
| SMILES | C1(S(N)(=O)=O)=C(Cl)C=CC(NC(NC2=CC=CC(Cl)=C2Cl)=O)=C1O |
| MFCD | N.A. |
| InChi | InChI=1S/C13H10Cl3N3O4S/c14-6-2-1-3-8(10(6)16)18-13(21)19-9-5-4-7(15)12(11(9)20)24(17,22)23/h1-5,20H,(H2,17,22,23)(H2,18,19,21) |
| InChiKey | WTLRWOHEKQGKDS-UHFFFAOYSA-N |
| CID | 9887803 |
| Short Description | CXCR2 antagonist |
References
- H Xu 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.
- PL Podolin et al. A potent and selective nonpeptide antagonist of CXCR2 inhibits acute and chronic models of arthritis in the rabbit. J Immunol. 2002 Dec 1;169(11):6435-44.
- JR White et al. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem. 1998 Apr 24;273(17):10095-8.
- Y Wang et al. Protease-activated receptor-1 protects rat astrocytes from apoptotic cell death via JNK-mediated release of the chemokine GRO/CINC-1. J Neurochem. 2006 Aug;98(4):1046-60.
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