Fezolinetant

Research use only, not for human use.

A potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6.

A potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6; exhibits high activity in LH inhibition, shows >2.5-log selectivity against NK1R and NK2R subtypes, proves >300-fold selective against related HPG axis receptors (KOR, GnRH, GnIH-R, GPR54).Other Indication Phase 2 Clinical(In Vitro):Fezolinetant (ESN364, 1 mg/kg, iv bolus) reversibly inhibits the regular, pulsatile secretion of LH in the ovarectomized ewe. ESN364 represses the pulse pattern of LH in all treated animals. ESN364 (5 mg/kg, p.o.) lowers plasma LH, but not FSH, in the castrated monkey. ESN364 (10, 25, 50 mg/kg, orally) also blocks the LH surge and decreases ovarian hormone levels throughout the menstrual cycle in monkeys.

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ESN-364 | ESN 364

GPCR/G Protein

Neurokinin Receptor

Neurokinin Receptor

Other Indications

Other Disease

1629229-37-3

358.3954

C16H15FN6OS

>98% (HPLC)

DMSO : ≥ 50 mg/mL 139.51 mM

O=C(C1=CC=C(F)C=C1)N2[C@H](C)C3=NN=C(C4=NC(C)=NS4)N3CC2

[(8R)-5,6-Dihydro-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl](4-fluorophenyl)methanone

(-20℃)

With Ice Pack

≥ 2 years