661472-41-9
661472-41-9 structure
- Name: Relamorelin
- Chemical Name: Relamorelin
- CAS Number: 661472-41-9
- Molecular Formula: C43H50N8O5S
- Molecular Weight: 790.973
- Catalog: Signaling Pathways GPCR/G Protein GHSR
- Create Date: 2018-06-13 08:15:35
- Modify Date: 2024-01-05 14:40:02
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Relamorelin (RM-131), a Ghrelin analog, is a potent ghrelin receptor agonist, with a Ki of 0.42 nM for GHS-1a. Relamorelin can promote food intake and adiposity in mice. Relamorelin can be used for the research of cachexia, gastroparesis, and gastric/intestinal dysmobility disorders[1][2][3].
| Name | Relamorelin |
|---|---|
| Synonyms |
3-(1-Benzothiophen-3-yl)-N-(4-piperidinylcarbonyl)-D-alanyltryptophyl-N-(4-carbamoyl-4-piperidinyl)phenylalaninamide
Phenylalaninamide, 3-benzo[b]thien-3-yl-N-(4-piperidinylcarbonyl)-D-alanyltryptophyl-N-[4-(aminocarbonyl)-4-piperidinyl]- Relamorelin UNII-BIW199E18V BIW199E18V [3-(1-benzothiophen-3-yl)-N-(piperidin-4-ylcarbonyl)-D-alanyl]-D-tryptophyl-L-phenylalanyl-(4-aminopiperidine-4-carboxamide) 3-(1-Benzothiophen-3-yl)-N-(4-piperidinylcarbonyl)-D-alanyl-D-tryptophyl-N-(4-carbamoyl-4-piperidinyl)-L-phenylalaninamide L-Phenylalaninamide, 3-benzo[b]thien-3-yl-N-(4-piperidinylcarbonyl)-D-alanyl-D-tryptophyl-N-[4-(aminocarbonyl)-4-piperidinyl]- |
| Description | Relamorelin (RM-131), a Ghrelin analog, is a potent ghrelin receptor agonist, with a Ki of 0.42 nM for GHS-1a. Relamorelin can promote food intake and adiposity in mice. Relamorelin can be used for the research of cachexia, gastroparesis, and gastric/intestinal dysmobility disorders[1][2][3]. |
|---|---|
| Related Catalog | |
| Target |
Ki: 0.42 nM (GHS-1a)[1] |
| In Vitro | Relamorelin shows ∼3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=1. 12 nM)[1]. Relamorelin is 6 times more potent (EC50=0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC50=4.2 nM) as assessed in vitro by calcium mobilization[1]. |
| In Vivo | Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) increases the food intake and weight gain in rats[1]. Relamorelin (50-500 nmol/kg/day; continuous infusion for 5 days) decreases the loss of body mass and fat mass[1]. RM-131 (250-500 nmol/kg; a single s.c.) stimulates acute food intake in wt but not growth hormone secretagogue receptor (GHR) ko mice[2]. Animal Model: F344/NTacfBR male rats implanted with tumor[1] Dosage: 50, 500 nmol/kg/day Administration: Continuous infusion at a rate of 0.5 μL/h for 5 d s.c. Result: Resulted in an increase in food intake (tumor/saline 41.4 g, tumor/BIM-28131 72.5 g) and weight gain (tumor/saline -10.3%, tumor/BIM-28131 +19.5%). |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 1216.2±65.0 °C at 760 mmHg |
| Molecular Formula | C43H50N8O5S |
| Molecular Weight | 790.973 |
| Flash Point | 689.3±34.3 °C |
| Exact Mass | 790.362488 |
| LogP | 5.22 |
| Vapour Pressure | 0.0±0.3 mmHg at 25°C |
| Index of Refraction | 1.692 |