| Description | Fezolinetant (ESN-364) is an antagonist of the neurokinin 3 receptor (NK3R). It is used for the treatment of menopausal hot flushes. |
| In vivo | ESN364 在所有受试动物中抑制LH的脉冲模式。ESN364 (10, 25, 50 mg/kg, 口服) 同时阻断LH激增并在整个月经周期内降低猴子的卵巢激素水平。ESN364 (5 mg/kg, p.o.) 能降低去势猴的血浆LH水平，但不影响FSH。Fezolinetant (1 mg/kg, iv bolus) 在去卵巢羊中可逆地抑制LH的规律、脉冲式分泌 [1]。 |
| Synonyms | ESN-364 |
| molecular weight | 358.39 |
| Molecular formula | C16H15FN6OS |
| CAS | 1629229-37-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10 mg/mL (27.9 mM), Sonication is recommended. |
| References | 1. Fraser GL, et al. 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. |
| Citations | 1. Xu W, Li G, Chen Y, et al.A novel antidiuretic hormone governs tumour-induced renal dysfunction.Nature.2023: 1-8. |