SB 225002

Bezeichnung:SB 225002

CAS-Nr182498-32-4

Englisch Name:SB 225002

CBNumberCB1455331

SummenformelC13H10BrN3O4

Molgewicht352.14

MOL-Datei182498-32-4.mol

SB 225002 physikalisch-chemischer Eigenschaften

Siedepunkt	401.6±45.0 °C(Predicted)
Dichte	1.793±0.06 g/cm3(Predicted)
storage temp.	room temp
Löslichkeit	Soluble to 100mM in DMSO and to 50mM in ethanol
Aggregatzustand	Yellow solid
pka	5.29±0.10(Predicted)
Farbe	white to beige
Sensitive	Moisture Sensitive
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
InChIKey	MQBZVUNNWUIPMK-UHFFFAOYSA-N
CAS Datenbank	182498-32-4

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3
HS Code	2921490090

Gefahreninformationscode (GHS)

SB 225002 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC₅₀ value of 22 nM. SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC₅₀ = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC₅₀ = 30 nM). Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.
Verwenden
SB 225002 is a potent and selective CXCR2 antagonist with the ability to inhibit interleukin IL-8 binding to CXCR2.
Definition
ChEBI: 1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea is a nitrophenol.
Biologische Aktivität
Potent and selective CXCR2 chemokine receptor antagonist (IC 50 = 22 nM) that displays > 150-fold selectivity over CXCR1 receptors. Causes inhibition of IL-8 and GRO α -mediated calcium mobilization in HL60 cells (IC 50 values are 8 and 10 nM respectively). Prevents IL-8-induced neutrophil chemotaxis in vitro and sequestration in vivo . Inhibits HIV replication in lymphocytes and macrophages.
Biochem/physiol Actions
SB-225002 is a potent nonpeptide inhibitor of chemokine receptor CXCR2 with an IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2 and > 150-fold selectivity over CXCR1 receptors. CXCR2 binds many different immune cell chemoattractants. SB-225002 is crucial for cancer progression and is involved in inflammatory diseases like COPD, rheumatoid arthritis, and ulcerative colitis.
Lager
Store at RT
Einzelnachweise
1) White et al. (1998), Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration; J. Biol. Chem. 273 10095 2) Du et al. (2013) SB225002 Promotes Mitotic Catastrophe in Chemo-Sensitive and -Resistant Ovarian Cancer Cells Independent of p53 Status In Vitro; PLoS One. 8 e54572 3) Shen et al. (2013), Interleukin-8 prevents oxidative stress-induced human endothelial cell senescence via telomerase activation; Int. Immunopharmacol. 16 261 4) Lane et al. (2001), Interleukin-8 Stimulates Human Immunodeficiency Virus Type 1 Replication and Is a Potential New target for Antiretroviral Therapy; J. Virol. 75 8195 5) Wu et al. (2015), CXCR2 is essential for cerebral endothelial activation and leukocyte recruitment during neuroinflammation; J. Neuroinflammation 12 98

SB 225002 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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