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SB290157 (trifluoroacetate)研究進

發(fā)布日期：2017-10-30   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/SB290157_trifluoroacetate.htmlSB290157 (trifluoroacetate)/a產(chǎn)品描述：SB290157 trif
<a href="https://www.medchemexpress.com/SB290157_trifluoroacetate.html">SB290157 (trifluoroacetate)</a>產(chǎn)品描述：SB290157 trifluoroacetate is a potent and selective <b>C3a</b> receptor antagonist with an <b>IC<sub>50</sub></b> of 200 nM.

IC50 & Target: IC50: 200 nM (C3a)<sup>[1]</sup>

<i><b>In Vitro:</b></i> SB 290157, functions as a competitive antagonist of <sup>125</sup>I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR), with an IC<sub>50</sub> of 200 nM. SB 290157 blocks C3a-induced C3aR internalization in a concentration-dependent manner and C3a-induced Ca<sup>2+</sup> mobilization in RBL-C3aR cells and human neutrophils with IC<sub>50</sub>s f 27.7 and 28 nM, respectively. SB 290157 is selective for the C3aR in that it does not antagonize the C5aR or six other chemotactic G protein-coupled receptors. SB 290157 also inhibits C3a-induced Ca<sup>2+</sup> mobilization of RBL-2H3 cells expressing the mouse and guinea pig C3aRs. It potently inhibits C3a-mediated ATP release from guinea pig platelets and inhibits C3a-induced potentiation of the c<br><br>
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