GlpBio

Fezolinetant (ESN-364)

目录号: GC30104纯度: >98.00%同义词: 非唑奈坦,ESN-364
Fezolinetant (ESN-364) 是一种神经激肽 3 受体 (NK3R) 的拮抗剂，用于治疗更年期潮热。
Fezolinetant (ESN-364)
Cas No.: 1629229-37-3
规格价格库存数量操作
1mg¥1,080.00现货
1
5mg¥2,340.00现货
1
10mg¥3,780.00现货
1
10mM (in 1mL DMSO)¥2,574.00现货
1
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文献被引

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    187(9):2288-2304 (2024)
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产品描述 Description

Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

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[1].

[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.

实验参考方法 Experimental Reference Method

Animal experiment:

On the day of the experiment, the NK3R antagonist ESN364 is formulated in physiological saline with 9% 2-hydroxypropyl-β-cyclodextrin at a concentration of 2 mg/mL. At 240 minutes after the initiation of blood sampling, ESN364 (1 mg/kg, n=5) or vehicle (n=5) is administered by an iv bolus injection at a dose volume of 0.5 mL/kg through the jugular cannulae, and the injected material is flushed into the animal with 5 mL of heparinized saline. Blood sampling resumes at the indicated intervals following this iv administration.

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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
1629229-37-3
同义词
非唑奈坦,ESN-364
SMILES
O=C(N1[C@H](C)C2=NN=C(C3=NC(C)=NS3)N2CC1)C4=CC=C(F)C=C4
分子式
C16H15FN6OS
分子量
358.39 g/mol
溶解性
DMSO : ≥ 50 mg/mL (139.51 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol