Fezolinetant (Synonyms: ESN-364)
目录号: PL07739 纯度: ≥98%
CAS No. :1629229-37-3
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中文名称
Fezolinetant
中文别名
非唑奈坦
英文名称
Fezolinetant
英文别名
Fezolinetant;83VNE45KXX;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;Fezolinetant [USAN];GTPL10422;BDBM50112244;WHO 10205;compound 3 [PMID:26191358];SB19658;Q27269455;(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;Methanone, ((8R)-5,6-
Cas No.
1629229-37-3
分子式
C16H15FN6Os
分子量
358.39
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Fezolinetant 是一种神经激肽-3 受体 (neurokinin 3 receptor) 拮抗剂,可用于更年期潮热的研究。
生物活性
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
性状
Solid
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 20 mg/mL (55.81 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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