Catalog No.
Product Name
Application
Product Information
Citations
- YIL 781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM)
- Lin D, .et al. , Endocrinology. , 2014, 155(7):2355-62 PMID: 24735326
- Anamorelin is currently under development for the management of non-small lung cancer associated cachexia/anorexia.
- Makito Miyake, .et al. , Cancers (Basel), 2020, Jul 17;12(7):E1942 PMID: 32709007
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GHSR agonist
Anamorelin (ONO-7643, RC-1291, ST-1291) is an orally active, high-affinity, selective agonist of theĀ ghrelin receptor with an EC50 value of 0.74 nM in the HEK293/GRLN FLIPR assay. Anamorelin is currently under development for the management of non-small lung cancer associated cachexia/anorexia.
- Josua Jordi, .et al. , Sci Adv, 2018, Oct; 4(10): eaav1966 PMID: 30402545
- Capromorelin functions as a growth hormone secretagogue and ghrelin mimetic which causes the body to secrete human growth hormone in a way usually seen at puberty and in young adulthood.
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GHSR stimulator
Anamorelin fumarate is a synthetic orally active ghrelin receptor agonist which is under development for the management of non-small lung cancer associated cachexia/anorexia. -
GHSR agonist
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a. -
ghrelin receptor inverse agonist
PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36. -
GHSR ligand
des-Gln14-Ghrelin is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM. -
GHS-R1a Inverse Agonist
AZ-GHS-38 is an orally active inverse agonist of the growth hormone secretagogue receptor 1a (GHS-R1a), exhibiting an IC50 of 6.7 nM. This compound effectively reduces food intake in wild-type mice, making it a valuable tool for anti-obesity research. Its central nervous system penetration facilitates investigations into the modulation of appetite and energy homeostasis. -
Growth Hormone Secretagogue
L-739943 is a potent, orally active growth hormone (GH) secretagogue that functions by stimulating GH release. With an ED50 value of 1 nM, L-739943 has demonstrated effectiveness in promoting GH secretion in beagle dogs. This compound is useful for investigating GH-related therapeutic applications and understanding GH-mediated physiological processes. -
GHSR Antagonist
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. -
GHSR Antagonist
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. -
GHSR Agonist
Macimorelin acetate is a growth hormone secretagogue receptor (GHSR) agonist that acts orally to stimulate growth hormone (GH) release. This compound is utilized in research related to adult growth hormone deficiency (AGHD) and cancer anorexia-cachexia syndrome (CACS). Its ability to promote GH release makes it a valuable tool for investigating conditions associated with altered GH levels. -
GHS-R1a Antagonist
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. -
GHSR Antagonist
JMV 2959 hydrochloride is a selective antagonist of the growth hormone secretagogue receptor 1a (GHS-R1a), exhibiting an IC50 of 32Ā±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. -
ASM Inhibitor
KARI 201 hydrochloride is a selective inhibitor of acid sphingomyelinase (ASM) with a competitive mechanism of action, exhibiting an IC50 of 338.3 nM. This compound is capable of penetrating the blood-brain barrier and has demonstrated potential in improving neuropathological features associated with Alzheimer's disease. KARI 201 hydrochloride serves as a valuable tool for research applications focused on neurodegenerative disorders and the modulation of sphingolipid metabolism. -
Growth Hormone Secretagogue Agonist
L-692429 is a benzolactam derivative functioning as a nonpeptidyl growth hormone secretagogue (GHS) agonist. It exhibits biological activity by binding to G protein-coupled receptors with a Ki of 63 nM, facilitating the release of growth hormone. This compound is useful in research applications focused on growth hormone regulation and metabolism. -
Anti-aging Agent, GHSR Activator
Emoghrelin is a ghrelin receptor (GHSR) activator that promotes growth hormone secretion, making it a valuable anti-aging agent. Isolated from the traditional medicinal plant Heshouwu (Polygonum multiflorum), Emoghrelin's mechanism supports various biological activities tied to growth and regeneration processes. This compound is of particular interest in aging research and studies focused on metabolic regulation and endocrine functions. -
GHSR Inverse Agonist
PF-04628935 is a potent inverse agonist of the ghrelin receptor (GHSR) with a reported IC50 of 4.6 nM. It demonstrates oral bioavailability of 43% in rat models and effectively penetrates the blood-brain barrier. This compound is valuable for research applications focused on stress and anxiety, providing insights into the role of ghrelin signaling in these physiological processes. -
GHS-R1a Agonist
L-692585 is a highly potent nonpeptidyl agonist of the growth hormone secretagogue receptor 1a (GHS-R1a), characterized by a Ki value of 0.8 nM. This compound directly stimulates somatotropes, leading to the release of growth hormone (GH). L-692585 is valuable for research into growth hormone regulation and its implications in metabolic disorders and growth deficiencies. -
Isomer of GSK1614343
(Ī±R,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. -
GHRHR Activator
Human growth hormone-releasing factor (GHRH) is a hypothalamic polypeptide that activates the growth hormone-releasing hormone receptor (GHRHR) in the anterior pituitary. Its primary mechanism involves stimulating the production and secretion of growth hormone (GH), which is critical for various physiological processes including growth and metabolism. This reagent is valuable for research applications focused on endocrinology, developmental biology, and metabolic disorders. -
GRF Superagonist
(D-Ala2)-GRF (1-29) amide (human) is a superagonist of Growth Hormone-Releasing Factor (GRF), demonstrating approximately 50 times the GH-releasing potency compared to GRF (1-29) in both pig and rat models. This compound is essential for studies focused on growth hormone modulation, metabolic research, and endocrine system regulation. Its enhanced activity makes it a valuable tool for exploring the physiological roles of growth hormone in various biological processes. -
GHSR Agonist
Relamorelin is a potent agonist of the growth hormone secretagogue receptor (GHSR), specifically targeting the GHS-1a receptor with a Ki of 0.42 nM. This pentapeptide ghrelin analog exhibits the ability to enhance growth hormone secretion and facilitate gastric emptying. Relamorelin is valuable for research applications in understanding and treating conditions such as cachexia, gastroparesis, and gastrointestinal dysmobility disorders. -
GHSR Agonist
Relamorelin acetate is a selective agonist for the growth hormone secretagogue receptor (GHSR), exhibiting a Ki value of 0.42 nM for the GHS-1a receptor. This pentapeptide ghrelin analog effectively increases growth hormone levels and enhances gastric emptying. Utilized in research, Relamorelin acetate shows promise for addressing conditions such as cachexia, gastroparesis, and various gastric or intestinal dysmotility disorders. -
GHSR Agonist
Ghrelin receptor full agonist-2 (compound 12j) is a potent agonist of the ghrelin receptor (GHSR), facilitating enhanced signaling through this target. This compound demonstrates significant biological activity associated with ghrelin's roles in appetite regulation, energy homeostasis, and growth hormone secretion. Its applications extend to studies investigating metabolic disorders, neuroendocrine functions, and potential therapeutic strategies in obesity and related conditions. -
GHSR Agonist
GSK894490A is a non-peptide agonist of the growth hormone secretagogue receptor (GHSR). It elicits biological activity by enhancing ghrelin signaling, thereby promoting growth hormone release. This compound is valuable for research focused on metabolic regulation, appetite modulation, and potential therapeutic targets for growth hormone-related disorders. -
GHS1a Antagonist
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. -
GHRH Analog
[His1,Nle27] GHRF (1-32), amide, human is a potent analog of growth hormone-releasing hormone (GHRH) that primarily targets the growth hormone secretagogue receptor (GHRHR). This compound exhibits strong receptor affinity, making it a valuable tool in research applications focused on growth hormone regulation and related metabolic processes. Its use may enhance studies related to pituitary function and endocrine signaling pathways. -
GHSR Agonist
BMS-604992 free base is a selective agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding with an inhibition constant (Ki) of 2.3 nM and potent functional activity, characterized by an EC50 value of 0.4 nM. This compound has been shown to effectively stimulate food intake in rodent models, making it a valuable tool for research in the fields of appetite regulation and metabolic disorders. -
Ghrelin Agonist
CP-464709 is a potent agonist of the ghrelin receptor, capable of crossing the blood-brain barrier. This compound induces a biphasic blood pressure response when administered intravenously and elicits a pressor response following intrathecal administration by activating pre-sympathetic neurons in the spinal cord. CP-464709 is valuable for research on cardiovascular conditions and the mechanisms regulating blood pressure dynamics. -
GHSR1a Agonist
PF-6870961 is a selective inverse agonist of the growth hormone secretagogue receptor 1a (GHSR1a). It demonstrates Ki values of 73.6 nM for human GHSR, 239 nM for rat GHSR, and 217 nM for canine GHSR. This compound effectively inhibits constitutive GHSR1a-induced inositol phosphate accumulation with an IC50 of 300 nM and also blocks Ī²-arrestin mobilization with an IC50 of 1.10 nM. PF-6870961 serves as a valuable tool in research focused on GHSR signaling pathways and their physiological roles. -
GH Secretagogue
L-163255 free base is an orally active spiropiperidine that functions as a growth hormone (GH) secretagogue. This compound has been shown to elevate plasma levels of insulin-like growth factor I (IGF-I), making it a valuable tool for research into GH regulation and its effects on various physiological processes. Its unique mechanism of action supports studies in endocrinology and metabolic research. -
GHSR
GHRF, mouse is a peptide composed of 44 amino acids that acts as a growth hormone-releasing factor primarily targeting GHSR. This reagent stimulates the release and synthesis of growth hormone, playing a crucial role in growth regulation and metabolic functions. It is widely utilized in research applications focusing on endocrinology, growth disorders, and the mechanisms of hormone action. -
GHSR
Obestatin (rat) is a 23-amino acid peptide encoded by the Ghrelin gene that primarily targets the G-protein coupled receptor 39 (GHSR). It plays a critical role in regulating food intake, inhibiting jejunal contractions, and promoting weight management. Additionally, obestatin exhibits anti-inflammatory, cardioprotective, and antioxidant properties, making it a valuable reagent for research in metabolic disorders and cardiovascular health. -
GHS-R1a Inverse Agonist
AZ-GHS-22 is a potent inverse agonist targeting the growth hormone secretagogue receptor type 1a (GHS-R1a) with an IC50 of 0.77 nM. This compound exhibits significant inhibition of receptor activity, making it a valuable tool for research into metabolic regulation and appetite control. AZ-GHS-22 is particularly useful for studies focused on obesity and related disorders, enabling exploration of the physiological roles of GHS-R1a in non-central nervous system contexts. -
GH Release Inducer
GHRF, porcine is a growth hormone releasing factor peptide that acts as a potent inducer of growth hormone (GH) release. By binding to the growth hormone secretagogue receptor (GHSR), it stimulates the secretion of GH from the anterior pituitary gland. This reagent is valuable in studies focused on growth hormone regulation, metabolic processes, and endocrine signaling pathways. -
GHSR Agonist
BMS-604992 is a selective, orally active agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding with a Ki of 2.3 nM and demonstrates potent functional activity with an EC50 of 0.4 nM. This compound has been shown to effectively stimulate food intake in rodent models, making it valuable for research in appetite regulation and metabolic studies. -
GHSR1a Agonist
PF-6870961 hydrochloride is a potent inverse agonist of GHSR1a, exhibiting Ki values of 73.6 nM for human GHSR, 239 nM for rat GHSR, and 217 nM for dog GHSR. It effectively inhibits GHSR1a-induced inositol phosphate (IP) accumulation with an IC50 of 300 nM and demonstrates a strong inhibition of constitutive GHSR1a Ī²-arrestin mobilization with an IC50 of 1.10 nM. This compound is relevant for research applications exploring the physiological roles of GHSR1a in metabolic and neuroendocrine processes. -
Growth Hormone-releasing Factor
GHRF, bovine (bGRF(1-44)-NH2) is a peptide that functions as the Growth Hormone-releasing Factor, stimulating the secretion of bovine growth hormone (GH). This compound is essential for studying GH release mechanisms and is utilized in research involving growth regulation and metabolic processes. Furthermore, GHRF, bovine exhibits a synergistic effect when combined with Hydrocortisone, enhancing its biological activity. -
Ghrelin Receptor Agonist
K-(D-1-Nal)-FwLL-NH2 is a potent inverse agonist of the ghrelin receptor, exhibiting a high affinity with an EC50 of 3.4 nM and a Ki of 4.9 nM. This compound is instrumental for studies related to obesity, providing valuable insights into the regulation of appetite and energy balance. Its specificity and efficacy make it a relevant tool for investigating the physiological and pathological roles of ghrelin signaling. -
GHSR Agonist
Macimorelin is a potent GHSR agonist that serves as a growth hormone secretagogue. It effectively stimulates the release of growth hormone, making it a valuable tool in the investigation of adult growth hormone deficiency (AGHD) and cancer anorexia-cachexia syndrome (CACS). This compound is instrumental in research aimed at understanding the physiological roles of growth hormone and its potential therapeutic applications in these conditions. -
GHSR Agonist
BMS-604992 dihydrochloride is a selective agonist of the growth hormone secretagogue receptor (GHSR), exhibiting high-affinity binding with a Ki of 2.3 nM and potent functional activity with an EC50 of 0.4 nM. This small-molecule compound has been shown to stimulate food intake in rodent models, making it a valuable tool for studies related to appetite regulation and metabolic disorders. Its distinctive mechanism and efficacy position BMS-604992 dihydrochloride as an important reagent for research in endocrinology and neurobiology. -
ASM Inhibitor
KARI 201 is a selective, brain-penetrant competitive inhibitor of acid sphingomyelinase (ASM), exhibiting an IC50 of 338.3 nM. This compound acts as a ghrelin receptor agonist and demonstrates significant potential in ameliorating neuropathological features associated with Alzheimer's disease. KARI 201 is valuable for research investigating the modulation of ASM activity and its implications in neurodegenerative disorders. -
GHS-R Agonist
BMS-317180 is a potent and orally active agonist of the growth hormone secretagogue receptor (GHS-R), with an EC50 of 7.9 nM. This compound effectively stimulates the endogenous release of growth hormone. BMS-317180 is suitable for research applications related to age-related frailty, osteoporosis, and cancer cachexia. -
Growth Hormone Receptor Antagonist
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. -
GHRH Antagonist
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. -
Growth Hormone-Releasing Factor
GHRF, ovine is a growth hormone-releasing factor that specifically stimulates the secretion of pituitary growth hormone (GH). It plays a crucial role in the physiological response to hypoglycemia, enhancing GH release to regulate metabolic processes. This reagent is utilized in research focused on growth hormone regulation, metabolic disorders, and endocrine system studies. -
Growth Hormone Secretagogue Agonist
L-692429 hydrochloride is a nonpeptidyl growth hormone secretagogue (GHS) agonist and a benzolactam derivative, primarily targeting the growth hormone secretagogue receptor. With a binding affinity characterized by a Ki of 63 nM, this compound effectively stimulates growth hormone release, making it valuable for studies in endocrine regulation and metabolic research. Its applications extend to investigating the physiological roles of growth hormone and exploring therapeutic avenues for growth-related disorders. -
Ghrelin Receptor Agonist
GSK894281 is a highly potent ghrelin receptor agonist exhibiting a pEC50 of <4.9 at the human motilin receptor. This compound demonstrates the ability to penetrate the central nervous system effectively. GSK894281 is primarily utilized in research applications related to gastrointestinal function, particularly for investigating therapies for constipation and facilitating colonic emptying prior to procedures such as colonoscopy or colon surgery.
