Fezolinetant-ESN-364-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFezolinetantCat. No.: HY-19632CAS No.: 1629229-37-3Synonyms: ESN-364分式: CHFNOS分量: 358.39作靶点: Neurokinin Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外

2、实验 DMSO : 50 mg/mL (139.51 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7903 mL 13.9513 mL 27.9026 mL5 mM 0.5581 mL 2.7903 mL 5.5805 mL10 mM 0.2790 mL 1.3951 mL 2.7903 mL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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清

3、的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.98 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.98 mM); Clear solution1/2 Maste

4、r of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.98 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Fezolinetant种神经激肽-3 受体 (neurokinin 3 receptor) 拮抗剂，可于更年期潮热的研究。体内研究 Fezolinetant (ESN364, 1 mg/kg, iv bolus) reversibly inhibits the regular, pulsatile secr

5、etion of LH in theovarectomized 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 blocksthe LH surge and decreases ovarian hormone levels throughout the menstrual

6、cycle in monkeys 1.PROTOCOLAnimal On the day of the experiment, the NK3R antagonist ESN364 is formulated in physiological saline with 9% 2-Administration 1 hydroxypropyl-cyclodextrin at a concentration of 2 mg/mL. At 240 minutes after the initiation of bloodsampling, ESN364 (1 mg/kg, n=5) or vehicle

7、 (n=5) is administered by an iv bolus injection at a dose volumeof 0.5 mL/kg through the jugular cannulae, and the injected material is flushed into the animal with 5 mL ofheparinized saline. Blood sampling resumes at the indicated intervals following this iv administration.MCE has not independently

8、 confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 J Allergy Clin Immunol. 2019 Aug.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Fraser GL, et al. The NK3 Receptor Antagonist ESN364 Interrupts Pulsatile LH Secretion and Moderates Levels of Ovarian HormonesThroughout the Menstrual Cycle. Endocrinology. 2015 Nov;156(11):4214-25.McePdfHeightCaution: Product has not been fully validated for medical applicat