FSH

MHY1485 是一种 mTOR 激活剂，具有细胞渗透性。MHY1485 抑制自噬体和溶酶体融合，导致 LC3II 蛋白的积累和自噬体增大，从而抑制细胞自噬。

Cyclofenil 是一种选择性雌激素受体调节剂和排卵诱导剂，具有抗登革热病毒活性。

Relugolix (RVT-601) 是口服有活性的非肽性促性腺激素释放激素的拮抗剂。同 TAK-013 相比，它对人和猴子的受体具有高亲和力和强拮抗活性，它们的 IC50值分别为0.33 nM 和0.32 nM。它可用于研究性激素依赖性疾病，如子宫肌瘤、子宫内膜异位症、前列腺癌等。

FSH receptor antagonist 1 (compound 10) 是一种高效的G(s)蛋白偶联人类促卵泡激素 (FSH) 受体拮抗剂，在表达人类FSH受体的细胞系中的IC50值为28 nM。该化合物在体外小鼠模型中显著抑制卵泡生长和排卵。

FSHreceptor-binding inhibitor fragment(bi-10) 是一种有效的 FSH 拮抗剂。FSHreceptor-binding inhibitor fragment(bi-10) 阻断 FSH 与 FSHR 的结合，并在受体水平上改变 FSH 的作用。FSHreceptor-binding inhibitor fragment(bi-10) 导致小鼠排卵抑制和卵泡闭锁。FSHreceptor-binding inhibitor fragment(bi-10) 通过下调卵巢中 FSHR 和 ERβ的过度表达来抑制卵巢癌发生。

Histrelin (Supprelin LA) 是促性腺激素释放激素 (GnRH) 的九肽类似物，具有增加的效力。它被认为是 GnRH 激动剂。 Histrelin 用于治疗对激素敏感的男性前列腺癌和女性子宫肌瘤。

FSHR agonist 1是一种对卵泡刺激素(FSH)受体(FSHR)具有高亲和力并能引起变构的激动剂，具有pEC50值为7.72。它通过与TMD广泛相互作用直接激活FSHR。

hFSH-β-(33-53) TFA 是一种含有硫醇的肽，对应于第二个 FSH 受体结合域，是 FSHR(卵泡刺激素受体) 拮抗剂。hFSH-β-(33-53) TFA 抑制 FSH 与受体的结合，是 Sertoli 细胞中雌二醇合成的部分激动剂。

Norgestrel (WY-3707) 是一种孕酮的合成类似物，是一种口服避孕药中常见的化合物，也是一种神经保护性强抗氧化剂，能够防止光诱导的感光细胞中的ROS 的生成以及细胞死亡。

Nafarelin acetate(76932-56-4 free base) (RS-94991-298) 是一种 GnRH 激动剂，可作为 GnRH 的类似物。 Nafarelin acetate(76932-56-4 free base) 导致促性腺激素促黄体激素 (LH) 和促卵泡激素 (FSH) 的垂体分泌减少。它可用于治疗雌激素依赖性病症。

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) 用作 GnRH 激动剂。它通过引起垂体的持续刺激来减少垂体促性腺激素促黄体激素 (LH) 和促卵泡激素 (FSH) 的分泌。曲普瑞林可用于治疗激素反应性癌症，如乳腺癌或前列腺癌、性早熟、雌激素依赖性疾病和辅助生殖。

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.

Coixol (MBOA) 是一种从薏苡仁中提取的多酚，有抗菌和抗肿瘤作用。

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).

Cetrorelix diacetate (NS-75A) 是GnRH 受体的强效拮抗剂(IC50:1.21 nM)。

Org 43553 是口服具有活力的低分子量 (LMW) 促黄体生成素受体(LH-R)激动剂，能够激动人 LH (EC50: 3.7 nM)和 FSH 受体(EC50: 110 nM) 。Org 43553 能够用于研究内分泌。

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是一种高效的KISS1R激动剂(IC50=170 pM)，改善了代谢稳定性。作为九肽metastin的类似物，对人和大鼠的EC50值分别为0.96 nM和1.6 nM。该化合物通过消耗下丘脑GnRH，能够降低血浆FSH、LH、睾酮水平，展示了对研究激素依赖性前列腺癌的潜力。

(D-Ser(tBu)6,D-Leu7,Azagly10)-LHRH是一种LHRH(黄体生成素释放激素)的类似物，主要通过激活垂体分泌黄体生成素(LH)和促卵泡激素(FSH)来在生殖调控中发挥核心作用。

(D-Ser4,D-Ser(tBu)6,Azagly10)-LHRH 是一种黄体生成素释放激素 (LHRH) 的类似物，主要通过促进垂体分泌黄体生成素 (LH) 和促卵泡激素 (FSH) 来在生殖调控中发挥关键作用。