RG7713-RO5028442-DataSheet-生命科学试剂-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作靶点: Vasopressin 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 : 20 mg/mL (45.6

2、7 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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

3、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 mg/mL (4.57 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2 mg/mL (4.57 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecu

4、les 您边的抑制剂师www.MedChemESolubility: 2 mg/mL (4.57 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 RG7713 (RO5028442)种效且有选择性的脑-渗透加压素 1a (V1a) 受体拮抗剂，其 Ki 值为 1 nM (hV1a)和 39 nM (mV1a)。IC50 & Target Ki: 1 nM (hV1a receptor), 39 nM (mV1a receptor) 1体外研究 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