gpr54

Kisspeptin-10, rat acetate(478507-53-8 free base) 是啮齿动物 Kisspeptin 受体 (KISS1, GPR54) 的内源性配体。

Kisspeptin 234 acetate(1145998-81-7 free base) 是Kisspeptin 受体 (KISS1, GPR54) 拮抗剂； 是Kisspeptin-10 类似物。它抑制 Kisspeptin-10 对磷酸肌醇 (IP) (IC50 = 7 nM) 的刺激和促性腺激素释放激素 (GnRH) 的释放。

Kisspeptin-10, human (TFA)(374675-21-5,FREE) 是一种有效的血管收缩剂和血管生成抑制剂。 Kisspeptin-10，人类 TFA 通过其受体 GPR54 充当肿瘤转移抑制因子。 Kisspeptin-10-GPR54系统在胚胎肾发育中发挥重要作用。 Kisspeptin-10 GPR54 信号通过 NFATc4 介导的 BMP2 表达诱导成骨细胞分化

TAK-683 TFA is a potent full agonist of the KISS1 receptor (KISS1R; IC50: 170 pM) with improved metabolic stability. It shows agonistic activities to KISS1R (EC50s: 0.96 nM and 1.6 nM for human and rat).

TAK-683 is an effective full KISS1 receptor agonist (IC50=170 pM). TAK-683 is a nonapeptide metastin analog, shows agonistic activities to KISS1R (EC50: 0.96 nM and 1.6 nM for human and rat, respectively).

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).

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..

Kisspeptin-10, human TFA为一种有效的血管收缩剂及血管生成抑制剂，通过其受体GPR54抑制肿瘤转移。Kisspeptin-10-GPR54系统对胚胎肾脏发展具有关键影响，而Kisspeptin-10 GPR54信号则通过NFATc4介导的BMP2表达促进成骨细胞分化。

Kisspeptin-54(human) TFA (Metastin(human) TFA) 是一种 Kisspeptin 受体 (KISS1，GPR54) 的内源性配体，以高亲和力结合大鼠和人类 GPR54受体，其Ki 值分别为 1.81 nM 和 1.45 nM。Kisspeptin-54(human) TFA 可抑制肿瘤转移并刺激促性腺激素分泌。

Kisspeptin-10, rat TFA 作为有效的血管收缩剂及血管生成抑制剂，为GPR54 (亦称KISS1) 亲吻蛋白受体的配体。此外，Kisspeptin-10, rat TFA 能降低Methotrexate引起的生殖毒性并显示出抗氧化潜力。

Kisspeptin 13 是一种 GPR54和 GnRH 受体激活剂，是一种内源性的活性异构体。Kisspeptin 13 能增强记忆，可用于阿尔茨海默病的研究。

Kisspeptin 234 TFA，作为一种十肽，是kisspeptin受体（KISS1, GPR54）的拮抗剂，并且是Kisspeptin 10的类似物。

Kisspeptin-10, rat is an Endogenous ligand for the rodent kisspeptin receptor (KISS1, GPR54).

Kisspeptin 234 is a kisspeptin receptor (KISS1, GPR54) antagonist; kisspeptin-10 analog. Inhibits kisspeptin-10 stimulation of inositol phosphate (IP) (IC50 = 7 nM) and release of gonadotrophin-releasing hormone (GnRH).

Potent endogenous ligand of the kisspeptin receptor (KISS1, GPR54). Binds with high affinity to rat and human KISS1 receptors with Ki values of 1.80 and 1.45 nM respectively. Inhibits chemotaxis, invasion and metastasis of human melanomas and breast carci

Endogenous ligand for the canine KISS1 receptor (Kisspeptin receptor or GPR54). Stimulates section of luteinizing hormone, follicle stimulating hormone and estradiol in vivo.

Kisspeptin-14 human 由 KiSS-1 基因编码，是一种与其他几种肽类激素共同由前体蛋白经不同蛋白酶切割而产生的肽类激素。该化合物保持和全长Kisspeptin相同的受体结合效率及效力，并通过与GPR54受体结合，激活该 G 蛋白偶联受体和多种细胞内信号传导途径。Kisspeptin-14 human 主要用于研究生殖发育和肿瘤转移。

Kiss2 peptide acetate 是 Kiss2 peptide 的醋酸盐版本，且作为一种积极的生殖调节剂发挥作用。该化合物在 COS-7 细胞中通过与其同源受体 Kiss2R (GPR54) 结合，通过 Gas 和 Gaq 蛋白激活相关的PKA和PKC信号通路，进而促进 cAMP 反应元件依赖性荧光素酶 (CRE-luc) 和血清反应元件依赖性荧光素酶 (SRE-luc) 的活性增强。