RG7713-RO5028442-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERG7713Cat. No.: HY-12981CAS No.: 920022-47-5Synonyms: RO5028442分式: CHClNO分量: 437.96作靶點: Vasopressin 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 : 20 mg/mL (45.6

2、7 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.2833 mL 11.4166 mL 22.8331 mL5 mM 0.4567 mL 2.2833 mL 4.5666 mL10 mM 0.2283 mL 1.1417 mL 2.2833 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?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，當天使；澄清的

3、儲備液可以根據(jù)儲存條件，適當保存；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 mg/mL (4.57 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2 mg/mL (4.57 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecu

4、les 您邊的抑制劑師www.MedChemESolubility: 2 mg/mL (4.57 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 RG7713 (RO5028442)種效且有選擇性的腦-滲透加壓素 1a (V1a) 受體拮抗劑，其 Ki 值為 1 nM (hV1a)和 39 nM (mV1a)。IC50 & Target Ki: 1 nM (hV1a receptor), 39 nM (mV1a receptor) 1體外研究 RG7713 (RO5028442) (compound 8) has excellent binding in a

5、nd functional affinity for hV1a, moderatemouse affinity, and excellent selectivity versus human V2 (hV2) and human oxytocin (hOT) receptors.RG7713 (RO5028442) shows high solubility. RG7713 (RO5028442) is found to be highly selective against apanel of 89 targets. Finally, RG7713 (RO5028442) is identi

6、fied as a suitable compound for clinical studies 1.PROTOCOLCell Assay 1 CHO cells are stably transfected with expression plasmids encoding human V1a and grown in F-12 K,containing 10% fetal bovine serum, 1% penicillin-streptomycin, 1% glutamate, and 200 g/mL geneticin at 37C in a 10% CO2 incubator a

7、t 95% humidity. Cells are plated for 24 h at 50,000 cells/well in clear bottomed96 well plates and are dye loaded for 60 min with 2 M Fluo-4-AM in assay buffer. After cell washing, theplate is loaded on a uorometricimaging plate reader, compound dilution series added to the cells, andagonist activit

8、y measured 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ratni H, et al. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via achemogenomic and scaffold hopping approach. J Med Chem. 2015 Mar 12;58(5):2275-89.McePdfHeightCaution: Product has not been fully validated for medical applicatio