Bioactivity | SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki 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]. |
Invitro | SB-209247(化合物 3)表现出对 LTB4 受体的高度选择性。SB-209247 在各自的受体结合测定中与 [3H]-fMLP 和 [3H]LTD4 竞争,IC50 值为 3250 nM 和 16800 nM,并与另外 14 种配体竞争,IC50 值大于 10000 nM。通过阻断 LTB4 诱导的 Ca2+ 动员和 LTB4 诱导的脱颗粒,在人多形核白细胞 (PMN) 中证明了细胞水平的功能活性,IC50 值分别为 6.6 nM 和 53 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> SB-209247 相关抗体: |
In Vivo | SB-209247(化合物 3)在小鼠模型中抑制中性粒细胞流入的 ED50 为 14.8 mg/kg,并抑制炎症反应的流体相(水肿),ED50 为 18.7 mg/kg[1] 。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 154413-61-3 |
Formula | C23H19Cl2NO3S |
Molar Mass | 460.37 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |