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MedKoo Cat#: 319660 | Name: Relamorelin

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Relamorelin, also known as BIM28131 and RM131, is a centrally penetrant, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) potentially useful for the treatment of diabetic gastroparesis, chronic idiopathic constipation, and anorexia nervosa. It is a pentapeptide and analogue of ghrelin with improved potency and pharmacokinetics. In humans, relamorelin produces increases in plasma growth hormone, prolactin, and cortisol levels, and, like other GHSR agonists, increases appetite.

Chemical Structure

Relamorelin
Relamorelin
CAS#661472-41-9

Theoretical Analysis

MedKoo Cat#: 319660

Name: Relamorelin

CAS#: 661472-41-9

Chemical Formula: C43H50N8O5S

Exact Mass: 790.3625

Molecular Weight: 790.98

Elemental Analysis: C, 65.29; H, 6.37; N, 14.17; O, 10.11; S, 4.05

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
BIM28131; BIM 28131; BIM-28131; BIM-28163; BIM 28163; BIM28163; RM131; RM-131; RM 131; Relamorelin
IUPAC/Chemical Name
N-((R)-3-(benzo[b]thiophen-3-yl)-1-(((R)-1-(((S)-1-((4-carbamoylpiperidin-4-yl)amino)-1-oxo-3-phenylpropan-2-yl)amino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-1-oxopropan-2-yl)piperidine-3-carboxamide
InChi Key
IPMQOGDSJZQLFX-BIBZJUPHSA-N
InChi Code
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
SMILES Code
O=C(C1(NC([C@@H](NC([C@H](NC([C@H](NC(C2CNCCC2)=O)CC3=CSC4=CC=CC=C34)=O)CC5=CNC6=C5C=CC=C6)=O)CC7=CC=CC=C7)=O)CCNCC1)N
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 790.98 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Camilleri M. Novel Diet, Drugs and Gastric Interventions for Gastroparesis. Clin Gastroenterol Hepatol. 2016 Jan 4. pii: S1542-3565(15)01724-3. doi: 10.1016/j.cgh.2015.12.033. [Epub ahead of print] Review. PubMed PMID: 26762845. 2: Bassotti G. Relamorelin to Treat Constipation: "Pusher" or Pushover? Dig Dis Sci. 2015 Oct 24. [Epub ahead of print] PubMed PMID: 26500115. 3: Acosta A, Camilleri M, Busciglio I, Boldingh A, Nelson AD, Burton D. Short-Term Effects of Relamorelin on Descending Colon Motility in Chronic Constipation: A Randomized, Controlled Trial. Dig Dis Sci. 2015 Oct 14. [Epub ahead of print] PubMed PMID: 26467700. 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. 5: Acosta A, Camilleri M, Kolar G, Iturrino J, Szarka LA, Boldingh A, Burton D, Ryks M, Rhoten D, Zinsmeister AR, Spence SC, Gottesdiener K, Bouras EP, Vazquez-Roque MI. Relamorelin Relieves Constipation and Accelerates Colonic Transit in a Phase 2, Placebo-Controlled, Randomized Trial. Clin Gastroenterol Hepatol. 2015 Dec;13(13):2312-2319.e1. doi: 10.1016/j.cgh.2015.04.184. Epub 2015 May 19. PubMed PMID: 26001337. 6: Shin A, Wo JM. Therapeutic applications of ghrelin agonists in the treatment of gastroparesis. Curr Gastroenterol Rep. 2015 Feb;17(2):430. doi: 10.1007/s11894-015-0430-8. Review. PubMed PMID: 25702264. 7: Acosta A, Camilleri M. Prokinetics in gastroparesis. Gastroenterol Clin North Am. 2015 Mar;44(1):97-111. doi: 10.1016/j.gtc.2014.11.008. Epub 2014 Dec 23. Review. PubMed PMID: 25667026. 8: Camilleri M, Acosta A. Emerging treatments in Neurogastroenterology: relamorelin: a novel gastrocolokinetic synthetic ghrelin agonist. Neurogastroenterol Motil. 2015 Mar;27(3):324-32. doi: 10.1111/nmo.12490. Epub 2014 Dec 29. Review. PubMed PMID: 25545036; PubMed Central PMCID: PMC4424792. 9: Peeters TL. Gastrointestinal hormones and gut motility. Curr Opin Endocrinol Diabetes Obes. 2015 Feb;22(1):9-13. doi: 10.1097/MED.0000000000000123. Review. PubMed PMID: 25517024. 10: Palus S, von Haehling S, Doehner W, Datta R, Zhang J, Dong JZ, Culler MD, Anker SD, Springer J. Effect of application route of the ghrelin analog BIM-28131 (RM-131) on body weight and body composition in a rat heart failure model. Int J Cardiol. 2013 Oct 3;168(3):2369-74. doi: 10.1016/j.ijcard.2013.01.263. Epub 2013 Mar 7. PubMed PMID: 23465234.