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.
Product information
CAS Number: 661472-41-9
Molecular Weight: 790.97
Formula: C43H50N8O5S
Chemical Name: 4-[(2S)-2-[(2R)-2-[(2R)-3-(1-benzothiophen-3-yl)-2-[(piperidin-3-yl)formamido]propanamido]-3-(1H-indol-3-yl)propanamido]-3-phenylpropanamido]piperidine-4-carboxamide
Smiles: NC(=O)C1(CCNCC1)NC(=O)[C@H](CC1C=CC=CC=1)NC(=O)[C@@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@@H](CC1=CSC2=CC=CC=C12)NC(=O)C1CNCCC1
InChiKey: IPMQOGDSJZQLFX-BIBZJUPHSA-N
InChi: InChI=1S/C43H50N8O5S/c44-42(56)43(16-19-45-20-17-43)51-41(55)34(21-27-9-2-1-3-10-27)49-39(53)35(22-29-25-47-33-14-6-4-12-31(29)33)50-40(54)36(48-38(52)28-11-8-18-46-24-28)23-30-26-57-37-15-7-5-13-32(30)37/h1-7,9-10,12-15,25-26,28,34-36,45-47H,8,11,16-24H2,(H2,44,56)(H,48,52)(H,49,53)(H,50,54)(H,51,55)/t28?,34-,35+,36+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Relamorelin shows ∼3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=1. 12 nM). 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.
In Vivo:
Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) increases the food intake and weight gain in rats. Relamorelin (50-500 nmol/kg/day; continuous infusion for 5 days) decreases the loss of body mass and fat mass. 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.
Products are for research use only. Not for human use.
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