Kisspeptin-54(human)  (Synonyms: Metastin(human))

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 K_i values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) inhibits tumor metastasis and stimulates the secretion of gonadotropin (LH) and testosterone^{[1][2][3][4][5][6][7][8]}.

Ki: 1.81 nM (Rat GPR54) and 1.45 nM (Human GPR54)^[2]

Kisspeptin-54(human) (1-100 nM, 4-48 h) stimulates aldosterone synthesis in human adrenal cells (H295R cells and fetal adrenal neocortex cells)^[3].
Kisspeptin-54(human) (1-10 μM, 12 h) suppresses migration of human pancreatic cancer cells (PANC-1) ^[4].
Kisspeptin-54(human) (10-1000 nM, 14-16 h for migration, 24-48 h for invasion) inhibits migration and invasion of human renal cell carcinoma cells (Caki-1 and ACHN) with overexpression of metastireceptor^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Kisspeptin-54(human) (0.3-100 nmol/kg, i.p., 30 min before trunk blood and anterior pituitaries are collected) dose-dependently shows activation of the anterior pituitary release of LH in post-pubertal male rats^[6].
Kisspeptin-54(human) (0.3-30 nmol/kg, i.p.) produces a dose-dependent effect on c-fos mRNA levels in the anterior pituitary in various ages (PND15, PND30, and PND45) male rats^[6].
Kisspeptin-54(human) (0.1-30 nmol/kg, i.p., single) increases serum testosterone in mice, with the same potency as for mouse kisspeptins^[7].
Kisspeptin-54(human) (6.7 nmol/rat, s.c.) induces the release of gonadotropin via activation of the hypothalamic GnRH neurons in prepubertal female rats^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

5857.43

C₂₅₈H₄₀₁N₇₉O₇₈

374683-24-6

Solid

White to off-white

Gly-Thr-Ser-Leu-Ser-Pro-Pro-Pro-Glu-Ser-Ser-Gly-Ser-Arg-Gln-Gln-Pro-Gly-Leu-Ser-Ala-Pro-His-Ser-Arg-Gln-Ile-Pro-Ala-Pro-Gln-Gly-Ala-Val-Leu-Val-Gln-Arg-Glu-Lys-Asp-Leu-Pro-Asn-Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2

GTSLSPPPESSGSRQQPGLSAPHSRQIPAPQGAVLVQREKDLPNYNWNSFGLRF-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. M L Gottsch, et al. A Role for Kisspeptins in the Regulation of Gonadotropin Secretion in the Mouse. Endocrinology. 2004 Sep;145(9):4073-7.  [Content Brief]

  [2]. M Kotani, et al. The Metastasis Suppressor Gene KiSS-1 Encodes Kisspeptins, the Natural Ligands of the Orphan G Protein-Coupled Receptor GPR54. J Biol Chem. 2001 Sep 14;276(37):34631-6.  [Content Brief]

  [3]. Nakamura Y, et al. Metastin stimulates aldosterone synthesis in human adrenal cells. Reprod Sci. 2007 Dec;14(8):836-45.  [Content Brief]

  [4]. Masui T, et al. Metastin and its variant forms suppress migration of pancreatic cancer cells. Biochem Biophys Res Commun. 2004 Feb 27;315(1):85-92.  [Content Brief]

  [5]. Shoji S, et al. Metastin inhibits migration and invasion of renal cell carcinoma with overexpression of metastin receptor. European urology, 2009, 55(2): 441-451.

  [6]. Bentsen AH, et al. Maturation of kisspeptinergic neurons coincides with puberty onset in male rats. Peptides. 2010 Feb;31(2):275-83.  [Content Brief]

  [7]. Mikkelsen JD, et al. Comparison of the effects of peripherally administered kisspeptins. Regul Pept. 2009 Jan 8;152(1-3):95-100.  [Content Brief]

  [8]. Matsui H, et al. Peripheral administration of metastin induces marked gonadotropin release and ovulation in the rat. Biochem Biophys Res Commun. 2004 Jul 23;320(2):383-8.  [Content Brief]