SB-209247 

SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a K_i of 0.78 nM. SB-209247 blocks LTB4-induced Ca²⁺ mobilization with an IC₅₀ of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity^[1].

SB-209247 (Compound 3) demonstrates a high degree of selectivity for the LTB4 receptor. SB-209247 competes with [³H]-fMLP and [³H]LTD4 in respective receptor binding assays with IC₅₀ values of 3250 nM and 16800 nM and with another 14 ligands with IC₅₀ values greater than 10000 nM. Functional activity at the cellular level is demonstrated in human polymorphonuclear leukocytes (PMNs) by blocking the LTB4-induced Ca²⁺ mobilization and LTB4-induced degranulation with IC₅₀ values of 6.6 nM and 53 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB-209247 (Compound 3) has an ED₅₀ of 14.8 mg/kg for inhibiting neutrophil influx in the murine model, and inhibits the fluid phase (edema) of the inflammatory response with an ED₅₀ of 18.7 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

460.37

C₂₃H₁₉Cl₂NO₃S

154413-61-3

O=C(O)/C=C/C1=NC(CSC2=C(Cl)C=CC=C2Cl)=CC=C1OCCC3=CC=CC=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. R A Daines, et al. (E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity. J Med Chem. 1996 Sep 13;39(19):3837-41.  [Content Brief]