gpr54

Kisspeptin-10, human TFA is a potent vasoconstrictor and angiogenesis inhibitor. Kisspeptin-10, human TFA acts as a tumor metastasis suppressor via its receptor GPR54. Kisspeptin-10-GPR54 system plays an important role in embryonic kidney development. Kisspeptin-10/GPR54 signaling induces osteoblast differentiation via NFATc4-mediated BMP2 expression

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

Kisspeptin 234 acetate(1145998-81-7 free base) is a Kisspeptin receptor (KISS1, GPR54) antagonist; a Kisspeptin-10 analogue. It inhibits the stimulation of inositol phosphate (IP) (IC50 = 7 nM) and the release of gonadotropin-releasing hormone (GnRH) by kisspeptin-10.

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, is a potent vasoconstrictor and angiogenesis inhibitor that also suppresses tumor metastasis through its interaction with the receptor GPR54. It is crucial for embryonic kidney development and promotes osteoblast differentiation through NFATc4-mediated BMP2 expression via the Kisspeptin-10/GPR54 signaling pathway [1].

Kisspeptin-54(human) TFA, also known as Metastin(human) TFA, is the natural ligand for the kisspeptin receptor (KISS1, GPR54). It demonstrates high affinity for both rat and human GPR54 receptors with dissociation constants (K i) of 1.81 nM and 1.45 nM, respectively. This compound plays a crucial role in inhibiting tumor metastasis and promoting the secretion of gonadotropins, as evidenced by references [1] [2].

Kisspeptin-10, rat TFA serves as both a potent vasoconstrictor and an inhibitor of angiogenesis, as well as acting as a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Additionally, Kisspeptin-10 TFA demonstrates potential antioxidant properties by reducing Methotrexate-induced reproductive toxicity [1].

Kisspeptin 13, an endogenous active isoform, serves as an activator for both GPR54 and GnRH receptors. It has been shown to enhance memory, rendering it a valuable tool in Alzheimer's disease research [1].

Kisspeptin 234 TFA is a 10-amino acid peptide analog of Kisspeptin 10 [1] that functions as an antagonist to the kisspeptin receptor (KISS1, GPR54).

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 is an active fragment peptide of Kisspeptin, comprising 14 amino acids encoded by the KiSS-1 gene. Kisspeptin-14 human acts as a GPR54 agonist, exhibiting Ki values of 1.65 and 2.04 nM for human and rat GPR54 receptors, respectively, in CHO-K1 cells, with corresponding EC50 values of 7.22 and 1.33 nM.

Kiss2 peptide acetate is the acetate form of Kiss2 peptide, serving as a positive regulator of reproduction. It binds to its homologous receptor Kiss2R (GPR54) in COS-7 cells, activating the PKA and PKC signaling pathways through Gas and Gaq proteins. This activation enhances the activity of both cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).

Kiss2 peptide functions as a positive regulator of reproductive behavior. In COS-7 cells, it binds to its homologous G-protein coupled receptor Kiss2R (GPR54), activating the PKA and PKC signaling pathways through Gas and Gaq proteins. This enhances the activity of cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).

Kisspeptin antagonist p271 is a Kisspeptin inhibitor with cell-penetrating properties. It blocks the binding of endogenous Kisspeptin to GPR54 on pituitary growth hormone cells, removing the inhibition on growth hormone secretion. This compound specifically and significantly stimulates the release of growth hormone while inhibiting luteinizing hormone, without affecting prolactin or cortisol levels. Kisspeptin antagonist p271 may be used in research related to growth hormone deficiency disorders.