fsh

MHY1485 is an mTOR activator that is cell-permeable. MHY1485 inhibits autophagosome and lysosome fusion, leading to accumulation of LC3II proteins and increased autophagosomes, thereby inhibiting cellular autophagy.

FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s) protein-coupled human follicle-stimulating hormone (FSH) receptor. It exhibits an IC50 value of 28 nM in cell lines expressing the human FSH receptor. This compound significantly inhibits follicle growth and ovulation in in vitro mouse models.

FSH receptor-binding inhibitor fragment (bi-10) is a potent antagonist that inhibits the binding of follicle-stimulating hormone (FSH) to its receptor (FSHR), modifying FSH activity at the receptor level. It suppresses ovulation and induces follicular atresia in mice. Furthermore, this compound holds potential for curbing ovarian cancer carcinogenesis by reducing the overexpression of FSHR and estrogen receptor beta (ERβ) in the ovaries [1].

FSHR agonist 1, an allosteric agonist of the follicle-stimulating hormone receptor (FSHR), exhibits high affinity, with a pEC50 of 7.72. It forms extensive interactions with the transmembrane domain (TMD) to directly activate FSHR.

hFSH-β-(33-53) TFA, a thiol-containing peptide representing the second follicle-stimulating hormone receptor (FSHR) binding domain, acts as an FSHR antagonist, preventing FSH from binding to its receptor and partially promoting estradiol synthesis in Sertoli cells [1] [2] [3].

Norgestrel (WY-3707) is a synthetic progestin commonly used alone or in combination with an estrogen for contraception. Norgestrel suppresses the secretion of luteinizing and follicle-stimulating hormones (LH and FSH), thickens cervical mucus, and slows the transit of ova through the fallopian tubes.

Cyclofenil is an estrogen antagonist, has anti-dengue-virus activity

Nafarelin is a gonadotropin-releasing hormone (GnRH) agonist. Nafarelin increases the release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) by the anterior pituitary leading to an increase of estrogen progesterone.

Histrelin (Supprelin LA) acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency. It is considered a GnRH agonist. Histrelin is used in the treatment of hormone-sensitive cancers of the prostate in men and uterine fibroids in women.

Nafarelin acetate(76932-56-4 free base) (RS-94991-298) is a GnRH agonist that acts as an analog of GnRH. Nafarelin acetate(76932-56-4 free base) causes a decrease in the pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It may be used in the treatment of estrogen-dependent conditions.

Clomifene is a selective estrogen receptor modulator (SERM), it has both estrogenic and anti-estrogenic activities. This agent causes the release of the pituitary gonadotropins follicle-stimulating hormone (FSH) and luteinizing hormone (LH), leading to ov

Triptorelin acetate(57773-63-4 free base) (CL 118,532) is used as a GnRH agonist. It decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by causing constant stimulation of the pituitary. Triptorelin acetate(57773-63-4 free base) may be used in the treatment of hormone-responsive cancers such as breast cancer or prostate cancer, precocious puberty, estrogen-dependent conditions, and assisted reproduction.

FW 34569 is an enkephalin analogue. It stimulated growth hormones and prolactin release and inhibited the release of cortisol and LH, while FSH remained unchanged.

1. Coixol (MBOA) acts as a central muscle relaxant with an anti-convulsant effect. 2. Coixol interacts with the pituitary to stimulate reproduction in voles. 3. Coixol has the ability to interact with FSH to stimulate follicular development and increase ovulation. 4. Coixol can regulate gene expression, production and secretion of mucin, by directly acting on airway epithelial cells.

Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.

Cetrorelix diacetate (NS-75A) is is a gonadotropin-releasing hormone antagonist. It works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

Org 43553 is an orally active, low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist that activates human LH receptors (EC50: 3.7 nM) and FSH receptors (EC50: 110 nM). Org 43553 can be used for endocrine studies.

Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. Nafarelin increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of estrogen progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will negatively feed back upon hypothalamus to decrease GnRH ( negative feedback loop ) Through negative feedback, Nafarelin causes a decrease in pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Nafarelin may be used in the treatment of estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat central precocious puberty, and to control ovarian stimulation in IVF. It is normally delivered via a nasal spray. Nafarelin acetate is marketed by Searle (now part of Pfizer) under the brand name Synarel.

Dicetrorelix pamoate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner. Cetrorelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner......

TAK-448 is an investigational oligopeptide analog of kisspeptin and a potent agonist of the GPR54 receptor. In animals, acute TAK-448 administration stimulates LH FSH release, whereas continuous sc exposure rapidly down-regulates the pituitary-gonadal axis, with rapid reduction of T levels in a dose-dependent manner. TAK-448 has exhibited potent antitumor activity in rat androgen-dependent prostate cancer models. Therefore, TAK-448 may be useful in the treatment of PC in humans..

Triptorelin, a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2), is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts. By causing constant stimulation of the pituitary, it decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, precocious puberty, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. It is also used as therapy for gender identity disorder.

TAK-683 acetate is a nonapeptide metastin analog and a potent full agonist of the KISS1 receptor (KISS1R), exhibiting IC 50 =170 pM and enhanced metabolic stability. This compound shows agonistic activities towards KISS1R, with EC 50 values of 0.96 nM and 1.6 nM for human and rat KISS1R, respectively. TAK-683 acetate effectively depletes GnRH in the hypothalamus and reduces plasma levels of FSH, LH, and testosterone in vivo, showcasing its potential for hormone-dependent prostate cancer research.

(D-Ser(tBu)6,D-Leu7,Azagly10)-LHRH, an analogue of luteinizing hormone-releasing hormone (LHRH), regulates reproductive processes by stimulating the secretion of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH) [1].