Fezolinetant

• CAT Number: I006784
• CAS Number: 1629229-37-3
• Molecular Formula: C16H15FN6OS
• Molecular Weight: 358.39
• Purity: ≥95%
• Synonyms: Fezolinetant; ESN-364; ESN 364; ESN364;(R)-(4-fluorophenyl)(8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone
• Target: Neurokinin-3 receptor antagonist
• Solubility: Soluble in DMSO
• Storage: 0 - 4°C for short term or -20 °C for long term
• IUPAC Name: (4-fluorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone
• InChI: InChI=1S/C16H15FN6OS/c1-9-13-19-20-14(15-18-10(2)21-25-15)23(13)8-7-22(9)16(24)11-3-5-12(17)6-4-11/h3-6,9H,7-8H2,1-2H3/t9-/m1/s1
• InChIKey: PPSNFPASKFYPMN-SECBINFHSA-N
• SMILES: O=C(C1=CC=C(F)C=C1)N2[C@H](C)C3=NN=C(C4=NC(C)=NS4)N3CC2

Fezolinetant (Cat.No:I006784), also known as ESN-364, is Neurokinin-3 (NK-3) receptor antagonist which has been optimized for use in women’s health, and is being developed for sex-hormone related disorders such as endometriosis, polycystic ovarian syndrome and uterine fibroids. Fexolinetant allows modulation of the hypothalamic-pituitary gonadal axis with a selective action on hormones relevant to disease. The agent is expected to have greater tolerability than competing products which target GnRH (Gonadotropin-releasing hormone).

Reference

1:Fraser GL, Ramael S, Hoveyda HR, Gheyle L, Combalbert J. The NK3 Receptor Antagonist ESN364 Suppresses Sex Hormones in Men and Women. J Clin Endocrinol Metab. 2016 Feb;101(2):417-26. doi: 10.1210/jc.2015-3621. Epub 2015 Dec 14. PubMed PMID: 26653113.2:Fraser GL, Hoveyda HR, Clarke IJ, Ramaswamy S, Plant TM, Rose C, Millar RP. The NK3 Receptor Antagonist ESN364 Interrupts Pulsatile LH Secretion and Moderates Levels of Ovarian Hormones Throughout the Menstrual Cycle. Endocrinology. 2015 Nov;156(11):4214-25. doi: 10.1210/en.2015-1409. Epub 2015 Aug 25. PubMed PMID: 26305889.