BAY-899 is an orally active and selective antagonist of the luteinizing hormone receptor (LH-R), exhibiting IC50 values of 185 nM and 46 nM for human LH (hLH) and rat LH (rLH) respectively. In vivo studies have demonstrated that BAY-899 effectively reduces sex hormone levels[1].
Lepidiline A (Macaline A) 是一种具有抗炎症活性的黄酮木质素。Lepidiline A 对HL-60细胞具有细胞毒活性,IC50值为 32.3 μM。它是从芸苔科植物Lepidium meyenii Walpers 的活性成分,可改善小鼠内源性性激素的平衡,提高果蝇的繁殖力。Lepidiline A 靶向HSD17B1基因的机制来增强酶的活性,提高性激素的生物转化效率,提高生殖能力。Lepidiline A 具有抗癌活性。
9(Z)-Pentacosene is a cuticular hydrocarbon and insect sex hormone.1,2,3 It is found in the cuticle of female F. canicularis flies and is an attractant to males in a trap assay.1 9(Z)-Pentacosene is a contact sex hormone in scarab beetles and locust borers that is more abundant in females than males.2,3 It elicits arrestment, alignment, and mounting by males of both species in mating assays but only elicits copulation by the locust borer. 9(Z)-Pentacosene is also produced by the orchid O. exaltata and by C. cunicularius, a pollinator of O. exaltata.4
Ozarelix is a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors. Mechanistically, LHRH antagonists exert rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones and would therefore be expected to be effective in a variety of hormonally dependent disease states including ovarian cancer, prostate cancer, BPH, infertility, uterine myoma and endometriosis. BPH is a non-cancerous enlargement of the prostate that is caused by testosterone. Unlike LHRH agonists, ozarelix has the potential to reduce testosterone just enough to reduce both prostate size and symptoms without the severe side effects associated with a reduction in testosterone.