Merotocin

Merotocin

Merotocin
Systematic (IUPAC) name
(3R,6S,9S,12S,15S)-6-(2-Amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
Identifiers
CAS Registry Number
ATC code None
PubChem CID:
ChemSpider
Synonyms N-(4-Sulfanylbutanoyl)-L-tyrosyl-L-isoleucyl-L-glutaminyl-L-asparaginyl-L-cysteinyl-N-[(4-fluorophenyl)methyl]glycyl-L-leucylglycinamide cyclic (1-5)-thioether
Chemical data
Formula C48H68FN11O12S
Molecular mass 1042.183423 g/mol

Merotocin (INN) (developmental code name FE-202767), also known as carba-1-(4-FBzlGly7)dOT, is a potent (EC50 < 0.1 nM) and highly selective (>1000-fold over the related vasopressin receptors) peptidic agonist of the oxytocin receptor that was derived from oxytocin.[1][2][3] It is under development by Ferring Pharmaceuticals for the treatment of preterm mothers with lactation failure requiring lactation support, and is in phase II clinical trials for this indication.[3]

See also

References

  1. ^ Manning, M.; Misicka, A.; Olma, A.; Bankowski, K.; Stoev, S.; Chini, B.; Durroux, T.; Mouillac, B.; Corbani, M.; Guillon, G. (2012). "Oxytocin and Vasopressin Agonists and Antagonists as Research Tools and Potential Therapeutics". Journal of Neuroendocrinology 24 (4): 609–628.  
  2. ^ Yang, Yang; Li, Hao; Ward, Richard; Gao, Linghuan; Wei, Ji-Fu; Xu, Tian-Rui (2014). "Novel oxytocin receptor agonists and antagonists: a patent review (2002 – 2013)". Expert Opinion on Therapeutic Patents 24 (1): 29–46.  
  3. ^ a b Wiśniewski K, Alagarsamy S, Galyean R, Tariga H, Thompson D, Ly B, Wiśniewska H, Qi S, Croston G, Laporte R, Rivière PJ, Schteingart CD (2014). "New, potent, and selective peptidic oxytocin receptor agonists" (PDF). J. Med. Chem. 57 (12): 5306–17.  

External links

  • Pipeline - Ferring Pharmaceuticals
  • Merotocin - AdisInsight