L-368-899-hydrochloride - Oxytocin Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEL-368,899 hydrochlorideCat. No.: HY-108677CAS No.: 160312-62-9分式: CHClNOS分量: 591.23作靶点: Oxytocin 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 : 130 mg/mL (219.88

2、 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.6914 mL 8.4569 mL 16.9139 mL5 mM 0.3383 mL 1.6914 mL 3.3828 mL10 mM 0.1691 mL 0.8457 mL 1.6914 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

3、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: 2.17 mg/mL (3.67 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.17 mg/mL (3.67 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.17 mg/m

4、L (3.67 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 L-368,899 hydrochloride种有效的，选择性的，可服的，肽类催产素受体 oxytocin receptor 拮抗剂，对和宫 oxytocin receptor 的 IC50 值分别为 8.9 nM 和 26 nM，为抗早产剂。IC50 & Target IC50: 8.9 nM (rat uterus oxytocin receptor), 26 nM (human uterus

5、oxytocin receptor) 1体外研究 L-368,899 hydrochloride is a potent, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50sof 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 is less activeon vasopressin receptor in human liver and kidney, rat l

6、iver and kidney (IC50, 510 nM, 960 nM, 890 nM,2400 nM, respectively) 1.REFERENCES1. Williams PD, et al. 1-(7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo 2.2.1-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing pretermlabor. J Med Chem. 1994 Mar 4;37(5):565-71.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Te