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首页-小分子抑制剂&激动剂-GPCR-Neurokinin Receptor-Fezolinetant
Fezolinetant

Chemical Structure : Fezolinetant

CAS No.: 1629229-37-3

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Fezolinetant (ESN-364, ESN364)

货号: PC-70195Not For Human Use, Lab Use Only.

Fezolinetant (ESN-364) is a potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6.

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5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Fezolinetant (ESN-364) is a potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6.
Fezolinetant (ESN-364) 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).

物理化学性质&存储条件

分子量 358.3954
分子式 C16H15FN6OS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

[(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

参考文献

1. Hoveyda HR, et al. ACS Med Chem Lett. 2015 May 19;6(7):736-40.

2. Fraser GL, et al. Endocrinology. 2015 Nov;156(11):4214-25.

3. Fraser GL, et al. J Clin Endocrinol Metab. 2016 Feb;101(2):417-26.

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