Relugolix-TAK-385-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERelugolixCat. No.: HY-16474CAS No.: 737789-87-6Synonyms: TAK-385分式: CHFNOS分量: 623.63作靶点: GNRH Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (80.18 mM;

2、Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.6035 mL 8.0176 mL 16.0351 mL5 mM 0.3207 mL 1.6035 mL 3.2070 mL10 mM 0.1604 mL 0.8018 mL 1.6035 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

3、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 (4.01 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 (4.01 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules

4、 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (4.01 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Relugolix个新颖的，肽的能够服的GnRH拮抗剂，IC50值是0.33 nM。REFERENCES1. MacLean DB et al. Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in HealthyMales.J Clin Endocrinol Me

5、tab. 2015 Dec;100(12):4579-87.2. Nakata D et al. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active,small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice. Eur J Pharmacol.2014 Jan 15;723:167-74.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 02