Relamorelin TFA is a pentapeptide ghrelin analog and a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for the GHS-1a receptor. It is centrally penetrant, increases growth hormone levels, and accelerates gastric emptying. This compound has potential for research into cachexia, gastroparesis, and gastric/intestinal dysmobility disorders.
- Pentapeptide ghrelin analog
- Selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist
- Ki of 0.42 nM for GHS-1a receptor
- Centrally penetrant
- Increases growth hormone levels
- Accelerates gastric emptying
- Shows ~3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=1.12 nM)
- 6 times more potent (EC50=0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC50=4.2 nM) in vitro by calcium mobilization
- Solid appearance, white to off-white color
- For research use only.