The anterior pituitary, pancreatic islets, thyroid gland, heart, and different parts of the brain have high expression levels of the seven transmembrane G protein-coupled receptor known as GHSR (growth hormone secretagogue receptor). GHS-R1a and GHS-R1b are the two types of GHS-R that are recognized as existing.
Gastric polypeptide ghrelin activates the GHS-R1a in the hypothalamus-pituitary axis, where it exhibits strong GH-releasing activity. When ghrelin or artificial peptidyl and non-peptidyl ghrelin-mimetic agents, known as GHS, bind to the GHS-R1a, a G-protein-coupled receptor, it preferentially couples to Gq, ultimately increasing the intracellular calcium content. Ghrelin and GHS also have significant effects on food intake, gut motility, sleep, memory, and behavior in addition to their powerful GH-releasing action. They also affect cardiovascular performance, cell proliferation, immune responses, and reproduction.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V4451 | PF-5190457 | 1334782-79-4 | PF-5190457 is a novel, potent, orally available and selective ghrelin receptor inverse agonist with a pKi of 8.36. |
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V75378 | PF-6870961 | 2857112-06-0 | PF-6870961 is an inverse agonist of GHSR1a with Kis of 73.6 nM (human GHSR), 239 nM (rat GHSR) and 217 nM (dog GHSR). |
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V75379 | PF-6870961 hydrochloride | 2857112-07-1 | PF-6870961 HCl is an inverse agonist of GHSR1a with Kis of 73.6 nM (human GHSR), 239 nM (rat GHSR) and 217 nM (dog GHSR). |
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V75370 | Relamorelin acetate (RM-131 acetate; BIM-28131 acetate) | 1809080-14-5 | Relamorelin (RM-131) acetate, a growth hormone analogue, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist/activator with a Ki of 0.42 for the GHS-1a receptor. |
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V75367 | Relamorelin TFA (RM-131 TFA; BIM-28131 TFA) | 2863659-22-5 | Relamorelin (RM-131) TFA, a auxin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist/activator with a Ki of 0.42 for the GHS-1a receptor. |
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V86607 | S1H | S1H is a mimetic of hGH and a human growth hormone receptor (hGHR) antagonist. | |
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V15925 | TC-G-1008 | 1621175-65-2 | TC-G-1008, formerly known as GPR39-C3, is a GPR39 (zinc receptor) agonist (EC50 are 0.4 and 0.8 nM for rat and human receptors respectively). |
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V75376 | YIL781 | 875258-85-8 | YIL781 is a potent, orally bioactive antagonist of the gastrointestinal ghrelin receptor (GHSR). |
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V2145 | Capromorelin | 193273-66-4 | Capromorelin, also known as CP-424,391, is a growth hormone secretagogue and ghrelin mimetic ( hGHS-R1a K(i)=7 nM, rat pituicyte EC(50)=3 nM). |
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V4077 | Ibutamoren mesylate | 159752-10-0 | Ibutamoren mesylate (formerly also known as MK-677, MK-0667, and L-163,191) is a novel, non-peptide, potent, long-acting, orally-active, and selective agonist of the ghrelin receptor and a growth hormone secretagogue (GHSR), mimicking the growth hormone (GH)-stimulating action of the endogenous hormone ghrelin. |
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V16403 | Capromorelin tartrate (CP-424,391) | 193273-69-7 | Capromorelin, formerly known as CP-424,391, is a growth hormone secretagogue and ghrelin mimetic ( hGHS-R1a K(i)=7 nM, rat pituicyte EC(50)=3 nM). |
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V4686 | Anamorelin | 249921-19-5 | Anamorelin (formerly also known as RC-1291 and ONO-7643) is a novel, potent, and orally bioavailable ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay. |
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