2. Relamorelin

Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research.

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Relamorelin Chemical Structure

Relamorelin Chemical Structure

CAS No. : 661472-41-9

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Relamorelin Related Antibodies

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Description

Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research[1][2][3][4].

IC50 & Target

Ki: 0.42 nM (GHS-1a)[1]
In Vitro

Relamorelin (RM-131) 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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Relamorelin Related Antibodies
In Vivo

Relamorelin (RM-131; 50-500 nmol/kg/day; s.c.; continuous infusion for 5 days) decreases the loss of body mass and fat mass. Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) increases the food intake and weight gain in rats[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: F344/NTacfBR male rats implanted with tumor[1]
Dosage: 50, 500 nmol/kg/day
Administration: SC; continuous infusion at a rate of 0.5 μL/h for 5 d
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%).
Clinical Trial
Molecular Weight

790.97

Formula

C43H50N8O5S
CAS No.
SMILES

O=C(C1CCNCC1)N[C@H](CC2=CSC3=CC=CC=C23)C(N[C@@H](C(N[C@@H](CC4=CC=CC=C4)C(NC5(CCNCC5)C(N)=O)=O)=O)CC6=CNC7=CC=CC=C67)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Relamorelin661472-41-9RM-131 BIM-28131RM131RM 131BIM28131BIM 28131BIM-28131Inhibitorinhibitorinhibit

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