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Relamorelin

Cat. No. M30443
Relamorelin Structure
Synonym:

RM-131; BIM-28131

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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 790.97
Formula C43H50N8O5S
CAS Number 661472-41-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Rajan Singh, et al. Front Pharmacol. Current Treatment Options and Therapeutic Insights for Gastrointestinal Dysmotility and Functional Gastrointestinal Disorders

[2] Madhusudan Grover, et al. Gut. Gastroparesis: a turning point in understanding and treatment

[3] H Zatorski, et al. J Physiol Pharmacol. Relamorelin and other ghrelin receptor agonists - future options for gastroparesis, functional dyspepsia and proton pump inhibitors-resistant non-erosive reflux disease

[4] Victor Chedid, et al. Expert Opin Investig Drugs. Relamorelin for the treatment of gastrointestinal motility disorders

[5] M Camilleri, et al. Neurogastroenterol Motil. Emerging treatments in Neurogastroenterology: relamorelin: a novel gastrocolokinetic synthetic ghrelin agonist

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Keywords: Relamorelin, RM-131; BIM-28131 supplier, Ghrelin Receptor/GHSR, inhibitors, activators


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