luteinizing hormone (human)

Luteinizing hormone (LH), a heterodimeric glycoprotein hormone synthesized by the pituitary gland, serves vital functions in human reproductive processes.

BAY-298 是一种口服有效且选择性的促黄体生成激素受体(LH-R)拮抗剂，分别针对hLH(人LH)、rLH(大鼠LH)和cLH(食蟹猴LH)展现出96 nM、23 nM和78 nM的IC50。作为一种纳摩尔级别的hLH-R拮抗剂，BAY-298 能够有效降低体内性激素水平。

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].

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).

Gonadorelin Acetate (33515-09-2 free base) (Luteinizing Hormone Releasing Hormone (LH-RH)) 是下丘脑神经肽，在控制生殖功能中起关键作用。

(R)-BAY-899 是一种 BAY-899 的 R 型异构体。其中 BAY-899 是一种选择性的、口服具有活力的促黄体生成激素受体 (LH-R) 拮抗剂，作用于 hLH (人 LH) (IC50: 185 nM) 和 rLH (大鼠 LH) (IC50: 46 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。

Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseline within seven days post-treatment. Formulations containing abarelix have previously been used in the treatment of advanced prostate cancer.

BAY 1214784是一种针对人促性腺激素释放激素受体(hGnRH-R)的高效、选择性口服活性拮抗剂，属于螺二氢吲哚衍生物化合物。该化合物能显著降低血浆促黄体激素水平，最高可达49%，同时显示出较低的药代动力学变异性和良好的耐受性，表现出研究子宫肌瘤的潜力。

GnRH Associated Peptide (GAP) (25-53), human 是来源于人的促性腺激素释放激素相关肽（GAP）的一个特定片段，具体为第25至第53位氨基酸（hGAP-25-53）。本片段可用作免疫原，用以产生含有MC-1、MC-2和MC-3等抗体的抗血清。GAP通过其内含的三个氨基酸加工位点，能与黄体生成素释放激素（LH-RH）序列进行有效连接。

GnRH Associated Peptide (GAP) (1-24), human 是人类的一个化合物，具体为促性腺激素释放激素相关肽(GAP)的第1至24个氨基酸片段(hGAP-1-24)。该化合物通过3个氨基酸加工位点与黄体生成素释放激素(LH-RH)序列连接。

(D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) 作为一种CRF拮抗剂，能有效阻断IL-1a诱发的黄体生成素 (LH) 抑制作用。

Human follicular gonadotropin releasing peptide (hF-GRP)是一种刺激垂体分泌促黄体激素(LH)及促卵泡激素(FSH)的激素类多肽，其作用可在体外实现。

Prostaglandin F2α serinol amide作为一种丝氨醇酰胺类G蛋白偶联受体，能够在人类非小细胞肺癌细胞中提高钙浓度。此外，Prostaglandin F2α在绵羊体内充当黄体溶解激素的角色，且可能作为脊髓伤害性介质存在。