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Relamorelin

Catalog No. T34281 CAS 661472-41-9

Synonyms: BIM28131, RM 131, BIM-28131, BIM-28163, BIM 28163, BIM28163, BIM 28131

Relamorelin (RM-131), a selective and potent growth hormone-releasing peptide/growth hormone secretagogue receptor (GHSR) agonist, is a potent growth hormone-releasing peptide mimetic with a high affinity for the GHS-1a receptor Relamorelin is a centrally permeable pentapeptide that increases growth hormone levels and accelerates gastric emptying and has potential for studying malignant disease.

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Relamorelin, CAS 661472-41-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 497.00
5 mg	In stock	$ 1,150.00
10 mg	In stock	$ 1,550.00
25 mg	In stock	$ 2,300.00
50 mg	In stock	$ 2,970.00
100 mg	In stock	$ 4,190.00

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Purity: 99.85%

ee: 100%

Purity: 95.28%

ee: 98.69%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Relamorelin (RM-131), a selective and potent growth hormone-releasing peptide/growth hormone secretagogue receptor (GHSR) agonist, is a potent growth hormone-releasing peptide mimetic with a high affinity for the GHS-1a receptor Relamorelin is a centrally permeable pentapeptide that increases growth hormone levels and accelerates gastric emptying and has potential for studying malignant disease.
Targets&IC50	GHS-1a:0.42 nM (Ki), native ghrelin:1.12 nM (Ki), native ghrelin:4.2 nM (EC50), GHS-1a receptor:0.71 nM (EC50)
In vitro	Relamorelin (RM-131) exhibits approximately 3 times greater affinity for GHS-1a (Ki=0.42 nM) compared to native ghrelin (Ki=1.12 nM). In vitro, as evaluated by calcium mobilization, Relamorelin is 6 times more potent (EC50=0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC50=4.2 nM)[2].
In vivo	Continuous infusion of Relamorelin (RM-131) at doses ranging from 50 to 500 nmol/kg/day via subcutaneous administration for 5 days results in a reduction in the loss of body mass and fat mass. In rats, when administered at a dose of 500 nmol/kg/day through continuous infusion for 5 days, Relamorelin increases food intake and promotes weight gain[1].A single subcutaneous injection of RM-131 at doses ranging from 250 to 500 nmol/kg stimulates acute food intake in wild-type mice but not in mice lacking the growth hormone secretagogue receptor (GHR)[1].

Synonyms	BIM28131, RM 131, BIM-28131, BIM-28163, BIM 28163, BIM28163, BIM 28131
Molecular Weight	790.97
Formula	C43H50N8O5S
CAS No.	661472-41-9

Storage

store at low temperature,keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (63.2 mM), Sonication is recommended.

References and Literature

1. Fischer K, et, al. The Pentapeptide RM-131 Promotes Food Intake and Adiposity in Wildtype Mice but Not in Mice Lacking the Ghrelin Receptor. Front Nutr. 2015 Jan 12;1:31. 2. DeBoer MD, et,al.Ghrelin treatment causes increased food intake and retention of lean body mass in a rat model of cancer cachexia. Endocrinology. 2007 Jun;148(6):3004-12. 3. Zatorski H, et, al. Relamorelin and other ghrelin receptor agonists - future options for gastroparesis, functional dyspepsia and proton pump inhibitors-resistant non-erosive reflux disease. J Physiol Pharmacol. 2017 Dec;68(6):797-805. 4. Sanger GJ, Furness JB. Ghrelin and motilin receptors as drug targets for gastrointestinal disorders. Nat Rev Gastroenterol Hepatol. 2016 Jan;13(1):38-48. doi: 10.1038/nrgastro.2015.163. Epub 2015 Sep 22. Review. PubMed PMID: 26392067.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Membrane Protein-targeted Compound Library

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Keywords

Relamorelin 661472-41-9 GPCR/G Protein GHSR BIM28131 RM 131 BIM-28131 BIM-28163 BIM 28163 BIM28163 BIM 28131 inhibitor inhibit

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