2. Signaling Pathways
  3. GPCR/G Protein
  4. Kisspeptin Receptor

Kisspeptin Receptor

Kiss1R; GPR54

The kisspeptin receptor, Kiss1R, also known as GPR54, is a G protein-coupled receptor (GPCR), and it was recognized as canonical receptor for the Kiss1-derived peptides, kisspeptins. Kisspeptins are a family of neuropeptides that are critical for initiating puberty and regulating ovulation in sexually mature females via the central control of the hypothalamic–pituitary–gonadal axis. Recent studies have shown that kisspeptin and Kiss1R are expressed in the mammalian ovary. Convincing evidence indicates that kisspeptins can activate a wide variety of signals via its binding to KISS1R. Experimental data gathered recently suggest a putative role of kisspeptin signaling in the direct control of ovarian function, including follicular development, oocyte maturation, steroidogenesis, and ovulation. Dysregulation or naturally occurring mutations of the kisspeptin/KISS1R system may negatively affect the ovarian function, leading to reproductive pathology or female infertility.

Kisspeptin Receptor Related Products (13):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P0076A
    TAK-448 acetate
    		98.87%
    TAK-448 acetate (MVT-602 acetate) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM.
    TAK-448 acetate
  • HY-P0254
    Kisspeptin-10, human
    		99.19%
    Kisspeptin-10, human is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10, human 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, human
  • HY-P0254A
    Kisspeptin-10, human TFA
    Kisspeptin-10, human TFA is a potent vasoconstrictor and inhibitor of angiogenesis. 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, human TFA
  • HY-P1196A
    Kisspeptin 234 TFA
    		Antagonist 98.92%
    Kisspeptin 234 TFA, is a 10 amino acid peptide as well as a kisspeptin receptor (KISS1, GPR54) antagonist. Kisspeptin 234 TFA is an analog of Kisspeptin 10.
    Kisspeptin 234 TFA
  • HY-P1197A
    Kisspeptin-10 (mouse, rat) (TFA)
    		99.91%
    Kisspeptin-10 (mouse, rat) TFA is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10 (mouse, rat) TFA is a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Kisspeptin-10 (mouse, rat) TFA reduces Methotrexate-induced reproductive toxicity as a potential antioxidant compound.
    Kisspeptin-10 (mouse, rat) (TFA)
  • HY-P10419
    Zebrafish Kisspeptin-1
    Zebrafish Kisspeptin-1 is the core sequence of the neuropeptide kisspeptin-1, which participate in the regulation of gonadotropin-releasing hormone (GnRH) release, and regulates the reproductive system.
    Zebrafish Kisspeptin-1
  • HY-P2161B
    TAK-683 acetate
    		99.91%
    TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
    TAK-683 acetate
  • HY-P0076
    TAK-448
    		99.90%
    TAK-448 (MVT-602) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM.
    TAK-448
  • HY-P2161A
    TAK-683 TFA
    TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
    TAK-683 TFA
  • HY-P10256
    Kiss2 peptide
    Kiss2 peptide is a positive regulator of reproduction by transducing its activity via PKA and PKC pathways, coupled with its cognate G protein-coupled receptor GPR54.
    Kiss2 peptide
  • HY-P1197
    Kisspeptin-10 (mouse, rat)
    Kisspeptin-10 (mouse, rat) is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10 (mouse, rat) is a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Kisspeptin-10 reduces Methotrexate-induced reproductive toxicity as a potential antioxidant compound.
    Kisspeptin-10 (mouse, rat)
  • HY-P2161
    TAK-683
    TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
    TAK-683
  • HY-P1196
    Kisspeptin 234
    		Antagonist
    Kisspeptin 234, is a 10 amino acid peptide as well as a kisspeptin receptor (KISS1, GPR54) antagonist. Kisspeptin 234 is an analog of Kisspeptin 10.
    Kisspeptin 234