TTNPB-Ro-13-7410-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETTNPBCat. No.: HY-15682CAS No.: 71441-28-6Synonyms: Ro 13-7410; Arotinoid acid; AGN191183分式: CHO分量: 348.48作靶點(diǎn): RAR/RXR作通路: Metabolic Enzyme/Protease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(shí)驗(yàn)

2、DMSO : 11.25 mg/mL (32.28 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.8696 mL 14.3480 mL 28.6961 mL5 mM 0.5739 mL 2.8696 mL 5.7392 mL10 mM 0.2870 mL 1.4348 mL 2.8696 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。BIOLOGICAL ACTIVITY物活性 TTNPB種有效的 RAR 激動劑。使RARs進(jìn)

3、競爭性結(jié)合實(shí)驗(yàn)中，作于RAR，RAR和RAR，IC50 分別為 5.1 nM，4.5 nM 和 9.3 nM。IC50 & Target IC50: 5.1 nM (RAR), 4.5 nM (RAR), 9.3 nM (RAR) 1體外研究TTNPB inhibits binding of 3HtRA with IC50s of 3.8 nM, 4 nM, and 4.5 nM for human RAR, , and ,1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemErespectively. TTNPB competes for 3HtR

4、A binding to CRABPI with IC50s of 1800 nM 1.PROTOCOLKinase Assay 1 Labeled and unlabeled retinoids are added to nucleosol or cytosolic fractions in ethanol so that the totalamount of ethanol added is constant in all tubes and did not exceed 2% of the incubation volume. Thereceptor preparations are i

5、ncubated with retinoids at 47C for 4-6 hr. Sephadex PD-10 desalting columns areused to separate bound radioligand from free radioligand after equilibrium is achieved. For competitivebinding assays, varying concentrations of unlabeled competing ligand are incubated with the appropriatenucleosol or cy

6、tosol in the presence of a fixed concentration of 3HtRA (sp act. 49.3 Ci/mmol) or 3H9-cisRA (sp. act. 24.0 Ci/mmol). Final concentrations of 3H tRA and 3H9-cis RA for nuclear receptor bindingassays are 5nM. Final concentrations of 3HtRA for CRABP binding assays is 30 nM. The IC50s arecalculated. For

7、 saturation kinetics, increasing concentrations of radiolabeled ligand (3HtRA sp. act. 49.3Ci/mmol, 3HTTNPB sp. act. 5.5 Ci/mmol) are added to the nucleosol of the appropriate receptor subtype inthe presence (nonspecific binding) or absence (total binding) of a 100-fold molar excess of the correspon

8、dingunlabeled retinoid. Specific binding is defined as the total binding minus nonspecific binding. Saturationkinetics are calculated 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Biomaterials. 2018 Dec 6;193:30-46. Patent. US20180263995

9、A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Pignatello MA, et al. Multiple factors contribute to the toxicity of the aromatic retinoid, TTNPB (Ro 13-7410): binding affinities anddisposition. Toxicol Appl Pharmacol. 1997 Feb;142(2):319-27.McePdfHeightCaution: Product has not been fully validated for medical