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. nM. Relamorelin TFA is a pentapeptide with centrally penetrating properties. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying, with potential for research into cachexia, gastroparesis, and gastric/intestinal motility disorders.

Physicochemical Properties

Molecular Formula	C45H51F3N8O7S
Molecular Weight	904.996059656143
Exact Mass	904.355
CAS #	2863659-22-5
Related CAS #	Relamorelin;661472-41-9;Relamorelin acetate;1809080-14-5
PubChem CID	162641838
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	9
Hydrogen Bond Acceptor Count	13
Rotatable Bond Count	15
Heavy Atom Count	64
Complexity	1480
Defined Atom Stereocenter Count	3
SMILES	C(C1=CNC2=CC=CC=C12)[C@H](C(=O)N[C@@H](CC1C=CC=CC=1)C(=O)NC1(CCNCC1)C(=O)N)NC(=O)[C@H](NC(C1CCNCC1)=O)CC1=CSC2=CC=CC=C12.C(F)(F)(F)C(=O)O
InChi Key	YKEWFQMJVBJGEJ-GTKQDQPASA-N
InChi Code	InChI=1S/C43H50N8O5S.C2HF3O2/c44-42(56)43(16-20-46-21-17-43)51-41(55)34(22-27-8-2-1-3-9-27)49-39(53)35(23-29-25-47-33-12-6-4-10-31(29)33)50-40(54)36(48-38(52)28-14-18-45-19-15-28)24-30-26-57-37-13-7-5-11-32(30)37;3-2(4,5)1(6)7/h1-13,25-26,28,34-36,45-47H,14-24H2,(H2,44,56)(H,48,52)(H,49,53)(H,50,54)(H,51,55);(H,6,7)/t34-,35+,36+;/m0./s1
Chemical Name	4-[[(2S)-2-[[(2R)-2-[[(2R)-3-(1-benzothiophen-3-yl)-2-(piperidine-4-carbonylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]piperidine-4-carboxamide;2,2,2-trifluoroacetic acid
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Ki: 0.42 nM (GHS-1a)[1]
ln Vitro	The affinity of relamorelin (RM-131) TFA for GHS-1a is almost three times higher than that of native ghrelin (Ki=1.12 nM; Ki=0.42 nM). In vitro calcium mobilization testing revealed that relamorelin TFA is six times more effective (EC50=0.71 nM) than native ghrelin (EC50=4.2 nM) at activating the GHS -1a receptor[1].
ln Vivo	Body mass and fat mass loss are lessened by relamorelin (RM-131; 50–500 nmol/kg/day; sc; continuous infusion for 5 days) TFA. Rats given relamorelin (500 nmol/kg/day; continuous infusion for 5 days) TFA eat more and gain more weight[1]. A single SC dose of RM-131 (250–500 nmol/kg) TFA increases acute food intake in wt mice, but not in GHR-KO mice.
Animal Protocol	Animal/Disease Models: F344/NTacfBR male rats implanted with tumor[1] Doses: 50, 500 nmol/kg/day Route of Administration: SC; continuous infusion at a rate of 0.5 μL/h for 5 d Experimental Results: 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	[1]. 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. [2]. 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. [3]. 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]. Nausea and Vomiting in 2021: A Comprehensive Update. J Clin Gastroenterol. 2021 Apr 1;55(4):279-299. [5]. Relamorelin for the treatment of gastrointestinal motility disorders. Expert Opin Investig Drugs. 2017 Oct;26(10):1189-1197.

Solubility Data

Solubility (In Vitro)	H2O: 100 mg/mL (110.50 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 50 mg/mL (55.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.1050 mL	5.5249 mL	11.0497 mL
	5 mM	0.2210 mL	1.1050 mL	2.2099 mL
	10 mM	0.1105 mL	0.5525 mL	1.1050 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.