Date published: 2025-11-9

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EPCR Activators

The class of EPCR activators comprises a diverse set of chemical compounds that directly or indirectly modulate the expression and function of Endothelial Protein C Receptor (EPCR). Notably, prostacyclin analogs like Iloprost and Forskolin exemplify direct activators by stimulating the prostacyclin receptor and adenylyl cyclase, respectively. These compounds elevate intracellular cAMP levels, serving as secondary messengers that activate downstream pathways intricately linked to EPCR, thereby providing a precise means of inducing cellular responses associated with EPCR activation. Cyclic AMP (cAMP) itself, as exemplified by direct administration or the use of analogs like 8-CPT-cAMP, stands as a central player in EPCR activation. Elevated cAMP levels directly activate various signaling cascades, offering a straightforward mechanism for influencing EPCR expression and function. Additionally, compounds such as PGE1, Isoproterenol, and Epinephrine exert their activating effects by engaging specific receptors and subsequently increasing cAMP levels, providing targeted approaches for inducing cellular responses associated with EPCR.

Furthermore, the class includes modulators like FTY720 and Milrinone, which act on Sphingosine-1-phosphate (S1P) receptors and PDE3, respectively. These compounds influence downstream signaling pathways, directly impacting EPCR expression and function. Their mechanisms involve the modulation of cellular responses linked to EPCR, demonstrating the multifaceted nature of EPCR activation. In summary, the class of EPCR activators encompasses a repertoire of chemical compounds that intricately modulate cellular pathways associated with EPCR. These activators act through well-defined mechanisms, offering a nuanced understanding of how specific biochemical and cellular pathways directly or indirectly influence the expression and activity of EPCR.

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