Date published: 2025-11-2

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GPR54 Activators

GPR54 activators represent a class of compounds designed to engage with GPR54, also known as the Kiss1 receptor, which is integral in metabolic and reproductive functions. Within this group, distinct compounds such as GnRH agonists like Leuprolide, are believed to interact with upstream regulators or downstream targets of GPR54, potentially influencing its activity via modulation of gonadotropin-releasing hormone activity. Similarly, GnRH antagonists like Cetrorelix may hold the ability to interact with GnRH receptors, potentially influencing the associated signaling pathways of GPR54. The modulation of other endocrine factors such as luteinizing hormone and follicle-stimulating hormone by agents like Clomiphene Citrate could also yield interactions with GPR54 signaling pathways.Other potential members of this class include Tamoxifen, an estrogen receptor modulator that could affect the expression or signaling of GPR54 by modulating estrogenic activity, and compounds like Medroxyprogesterone Acetate, which may impact GPR54 activity by interacting with progesterone receptors and modulating related signaling pathways. Agents like Enzalutamide, an androgen receptor modulator, by altering androgenic activity, could also have ramifications on the signaling or expression of GPR54. Furthermore, compounds like Forskolin that increase cAMP levels, and others like Sildenafil, that inhibit the degradation of cAMP or cGMP, might hold potential in influencing the signaling cascades and pathways related to GPR54.

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