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 Antagonists (2)

Kisspeptin Receptor Related Products (16):

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.

HY-P0254

Kisspeptin-10, human		99.68%
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.

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.

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.

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.

HY-P10489

Kisspeptin-14 human		99.84%
Kisspeptin-14 human is a peptide hormone encoded by the KiSS-1 gene. Kisspeptin-14 human, along with several other similar peptide hormones, is produced from a common precursor protein by cleavage by different proteases. Kisspeptin-14 human has the same receptor binding efficiency and potency as full-length kisspeptin. Kisspeptin-14 human binds to its receptor GPR54 and is able to activate this G protein-coupled receptor and activate multiple intracellular signaling pathways. Kisspeptin-14 human can be used to study reproductive development and tumor metastasis.

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.

HY-P10256A

Kiss2 peptide acetate
Kiss2 peptide acetate is the acetate form of Kiss2 pepride (HY-P10256). Kiss2 peptide acetate is a positive regulator of reproduction. Kiss2 peptide acetate binds with its cognate receptor Kiss2R (GPR54) in COS-7 cells, activates PKA and PKC signaling pathways through Gas and Gaq proteins, and thus enhances the activity of cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).

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.

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.

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.

HY-P10256

Kiss2 peptide
Kiss2 peptide is a positive regulator of reproduction. Kiss2 peptide binds with its cognate receptor Kiss2R (GPR54) in COS-7 cells, activates PKA and PKC signaling pathways through Gas and Gaq proteins, and thus enhances the activity of cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).

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.

HY-P2191

KISS1-305
KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and a chemical probe. KISS1-305 has suboptimal KISS1R agonistic activity, and resists plasma protease degradation.

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.

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.

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