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作靶點: Oxytocin Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 130 mg/mL (219.88

2、 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲

3、備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.17 mg/mL (3.67 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.17 mg/mL (3.67 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.17 mg/m

4、L (3.67 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 L-368,899 hydrochloride種有效的，選擇性的，可服的，肽類催產(chǎn)素受體 oxytocin receptor 拮抗劑，對和宮 oxytocin receptor 的 IC50 值分別為 8.9 nM 和 26 nM，為抗早產(chǎn)劑。IC50 & Target IC50: 8.9 nM (rat uterus oxytocin receptor), 26 nM (human uterus

5、oxytocin receptor) 1體外研究 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