Goserelin (ICI 118630) acetate is an injectable gonadotropin releasing hormone superagonist (GnRH agonist).IC50 value:Target: GnRH agonistGoserelin is used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty. It may also be used in the treatment of male-to-female transsexuals and is favoured above other anti-androgens in some countries, such as the UK. It is available as a 1-month depot and a long-acting 3-month depot. Goserelin stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner.
LH-RH (7-10) is a tetrapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (7-10) produced in macrophages, type I-like and type II pneumocytes[3].
Lamprey LH-RH I is a gonadotropin-releasing hormone, elevates plasma steroid levels and stimulates ovulation in the lamprey without biological activity in other animal models[1].
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).Target: GnRHin vitro: Elagolix is a short-acting, nonpeptide, GnRH antagonist, administered orally, that unlike injectable depot GnRH agonists and antagonists, produces a dose-dependent suppression of ovarian estrogen production, that is, from partial suppression at lower doses to full suppression at higher doses. Elagolix is regarded as the frontrunner of a new class of GnRH inhibitors that have been denoted as second-generation, due to their non-peptide nature and oral bioavailability.
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (salmon) is a GnRH analog that induces ovulation and/or spawning in farmed fish[1].
Nafarelin is a gonadotropin-releasing hormone (GnRH) agonist that stimulates secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Sequence: {Glp}-His-Trp-Ser-Tyr-{2-Naph-Ala}-Leu-Arg-Pro-Gly-NH2.
Bim 21009 is an inhibitor of gonadorelin.
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
sGnRH-A is a salmon gonadotropin-releasing hormone (GnRH) analogue that stimulates growth hormone secretion and can also be used as an inducer of ovulation by artificial insemination[1][2].
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (Surfagon, Mwt 1167.34 Da) is an agonist of gonadotropin-releasing hormone (GnRH). (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH can be used as an internal standard for the LC-MS analysis of leuprorelide acetate. (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH has potential applications in biochemical analysis and fertility[1][2][3].
Deslorelin is a GnRH agonist. Deslorelin implants can be used as an alternative to dopamine agonists to induce fertil eoestrus in the bitch in anoestrus. The deslorelin implant can be used successfully in the queen for oestrus inhibition. Deslorelin acetate did not significantly affect the spontaneous contraction amplitude but caused a decrease in the frequency in the dorsal and ventral parts of the bladder.
Triptorelin is a GnRH agaonist shown to inhibit estradiol-induced cancer cell proliferationIn vivo: (1) Triptorelin can improve the pregnancy rate by 12% to 15% in ewes6 and downregulate ovarian GnRHR-I expression of female rats, especially in late-growing follicles.(2) Triptorelin immunity blocked EET and UWT, inhibited uterine growth and development and enhance the expression levels s of ESR1, LHR, and FSHR proteins.
Abarelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
Fluorogestone acetate is a progesterone compound. Fluorogestone acetate inhibits ovulation and synchronizes the estrous cycle in cattle by inhibiting the release of luteinizing hormone (LH) from the pituitary gland[1].
Triptorelin acetate is a Gonadotropin-releasing hormone (GnRH) receptor agonist[1].
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion[1][2].
Ganirelix acetate (Ganirest) is an injectable competitive gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate directly competes against the endogenous molecule for receptor binding, and causes a rapid reduction in estradiol levels. Ganirelix acetate can be used for researching ovarian hyperstimulation syndrome (OHSS)[1].
BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively[1].
AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone[1].
Lecirelin is a synthetic gonadotropin-releasing hormone (GnRH) analogue. Lecirelin is widely used for the research of bovine ovarian follicular cysts[1].
Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.target: GnRH [1]IC50: 0.33 nM [1]In vivo: In female knock-in mice, twice-daily oral administration of TAK-385 (100mg/kg) induces constant diestrous phases within the first week, decreases the uterus weight to ovariectomized levels and downregulated GnRH receptor mRNA in the pituitary after 4 weeks.[2]
[D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a GnRH receptor agonist[1].
LH-RH (4-10) is a heptapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (4-10) produced in macrophages and type II pneumocytes[1].
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model[1][2].
Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist[1].
GnRH Associated Peptide (GAP) (25-53), human is the human gonadotropin-releasing hormone-associated peptide (GAP) 25-53 fragment (hGAP-25-53), can be used as immunogen to generate antiseras including MC-1, MC-2, and MC-3. GAP is joined to the luteinizing hormone-releasing hormone (LH-RH) sequence by a 3 amino acid processing site[1].
Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM[1].
LHRH, the luteinizing hormone-releasing hormone, is a neuropeptide hypothalamic. LHRH regulates reproduction. LHRH can be used for the research of cancer[1].
Leuprolide acetate is a potent gonadotropin-releasing hormone receptor agonist used for the treatment of prostate cancer, endometriosis, uterine fibroids.
(D-Trp6)-LHRH free acid is a luteinizing hormone-releasing hormone (LHRH) agonist[1].