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. |
|
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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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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V50978 | YIL-781 HCl | 1640226-17-0 | ghrelin receptor (GHS-R1a) antagonist |
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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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