GHSR

Ghrelin receptor agonists and antagonists act on the growth hormone secretagogue receptor (GHSR). The receptor was cloned in 1996 from pituitary and hypothalamus as the target of synthetic growth hormone secretagogues. Its endogenous ligand, ghrelin, was identified in 1999 as an acylated stomach peptide that releases growth hormone. GHSR signaling links growth hormone release with appetite and energy balance, which makes the receptor a frequent subject in metabolism research. Anamorelin, capromorelin and ulimorelin are small-molecule GHSR agonists, and des-Gln14-Ghrelin is a natural ghrelin variant. PF-5190457 acts as an inverse agonist, while liver-expressed antimicrobial peptide 2 (LEAP-2) antagonizes the receptor.

12 Items

  • YIL 781
    Cat. No.
    A11979

    YIL 781

    YIL 781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM)

    1 mg
    $35.00
    5 mg
    $90.00
    All 7 sizes
  • LEAP-2
    Cat. No.
    A26273

    LEAP-2

    Synonyms: Human liver expressed antimicrobial peptide-2

    LEAP-2 is a GHS-R1a antagonist with a reported IC50 of 6.0 nM. This peptide effectively suppresses the orexigenic effects of ghrelin, attenuating ghrelin-induced growth hormone release and reducing basal food intake. Additionally, LEAP-2 demonstrates antimicrobial activity against various microbial model organisms. This compound is useful for research applications focused on obesity, metabolic disorders, and infectious diseases.

    1 mg
    $100.00
    5 mg
    $255.00
    All 3 sizes
  • YIL781 hydrochloride
    Cat. No.
    A60535

    YIL781 hydrochloride

    YIL781 hydrochloride is a potent antagonist of the ghrelin receptor (GHSR). This compound has been shown to significantly improve glucose homeostasis in rat models, demonstrating its potential in metabolic research. YIL781 hydrochloride effectively inhibits the calcium response triggered by ghrelin, with pIC50 values of 7.90 and 8.27, indicating robust bioactivity in a research context.

    2 mg
    $65.00
    5 mg
    $105.00
    All 5 sizes
  • JMV 2959
    Cat. No.
    A60536

    JMV 2959

    JMV 2959 is an antagonist of the growth hormone secretagogue receptor type 1a (GHS-R1a), exhibiting an IC50 value of 32 nM. This compound is utilized in research aimed at elucidating the roles of GHS-R1a in growth hormone regulation and metabolic processes. Its potent inhibitory activity makes it a valuable tool for studies related to obesity, metabolic disorders, and the endocrine system.

    5 mg
    $90.00
    10 mg
    $160.00
    All 5 sizes
  • Cortistatin-8
    Cat. No.
    A60539

    Cortistatin-8

    Synonyms: PCFWKTCK

    Cortistatin-8 (CST-8; PCFWKTCK) is a synthetic analogue of the neuropeptide cortistatin that acts as an antagonist of the ghrelin receptor (GHS-R1a). This compound counteracts the effects of ghrelin on gastric acid secretion and influences growth hormone release from somatotroph cells. With no binding affinity for somatostatin receptors (SST-R), Cortistatin-8 is specifically designed for research applications investigating the modulation of ghrelin signaling both in vitro and in vivo.

    1 mg
    $80.00
    5 mg
    $180.00
    All 3 sizes
  • JMV 2959 hydrochloride
    Cat. No.
    A60540

    JMV 2959 hydrochloride

    JMV 2959 hydrochloride is a selective antagonist of the growth hormone secretagogue receptor 1a (GHS-R1a), exhibiting an IC50 of 32±3 nM in LLC-PK1 cellular assays. This compound is valuable for studies investigating the modulation of growth hormone release and its implications in metabolic disorders, obesity, and appetite regulation. Its efficacy as a GHS-R1a antagonist makes it a potent tool for exploring the signaling pathways associated with this receptor.

    1 mg
    $30.00
    5 mg
    $65.00
    All 6 sizes
  • (αR,8aS)-GSK1614343
    Cat. No.
    A60546

    (αR,8aS)-GSK1614343

    (αR,8aS)-GSK1614343 is an isomer of GSK1614343, acting as a potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. This compound effectively modulates the GH secretagogue pathway, making it valuable for research focused on obesity, metabolism, and growth-related disorders. Its distinct isomeric configuration provides unique properties for investigations into receptor biology and therapeutic target validation.

    5 mg
    $80.00
    10 mg
    $135.00
    All 5 sizes
  • GSK1614343
    Cat. No.
    A60554

    GSK1614343

    GSK1614343 is a selective antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. It effectively inhibits the calcium response induced by ghrelin, exhibiting a pIC50 value of 7.90. This compound serves as a valuable tool for exploring the physiological roles of the ghrelin signaling pathway in various research applications, particularly in rodent models.

    Out of stock

    All 3 sizes
  • Tezusomant
    Cat. No.
    A60573

    Tezusomant

    Tezusomant is a growth hormone receptor antagonist that effectively inhibits the activity of growth hormone. This compound is instrumental in investigating conditions related to excessive growth hormone secretion, such as acromegaly and related endocrine disorders. Tezusomant facilitates research aimed at understanding the underlying mechanisms of these diseases and exploring potential therapeutic interventions.

    Out of stock

    All 3 sizes
  • JV-1-36
    Cat. No.
    A60574

    JV-1-36

    JV-1-36 is a growth hormone-releasing hormone (GHRH) antagonist. This compound effectively inhibits the production of reactive oxygen species in A549 lung cancer cells, making it a valuable tool for investigating the biological effects of GHRH antagonists. Research applications include in vitro studies focused on cancer biology and role of GHRH in tumorigenesis.

    Out of stock

    All 3 sizes
  • JMV 3002
    Cat. No.
    A60578

    JMV 3002

    JMV 3002 is a potent antagonist of the growth hormone secretagogue receptor (GHSR). It exhibits significant biological activity by inhibiting hexarelin-stimulated food intake in rat models, achieving up to 98% reduction at a dose of 80 μg/kg. JMV 3002 does not induce release of growth hormone on its own, nor does it inhibit hexarelin-stimulated growth hormone secretion in infant rats at a dose of 160 μg/kg. This compound is valuable for research focused on energy homeostasis and the regulation of appetite.

    0.1 mg
    $105.00
    0.5 mg
    $455.00
    All 4 sizes
  • JMV 3008
    Cat. No.
    A60580

    JMV 3008

    JMV 3008 is a GHS-R1a antagonist with an IC50 of 5.6 nM, effectively inhibiting the growth hormone secretagogue receptor 1a. This compound demonstrates potential in the study of metabolic disorders, including diabetes and obesity, by modulating appetite and energy homeostasis. Research involving JMV 3008 can contribute valuable insights into therapeutic strategies targeting these diseases.

    25 mg
    $1,275.00
    All 1 sizes

12 Items

Added to your cart

View Cart Checkout

    Loading...