Puromycin-aminonucleoside-NSC-3056-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPuromycin aminonucleosideCat. No.: HY-15695CAS No.: 58-60-6Synonyms: NSC 3056分式: CHNO分量: 294.31作靶點(diǎn): Bacterial作通路: Anti-infection儲(chǔ)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) H2O : 33.33 mg/mL (1

2、13.25 mM; Need ultrasonic)DMSO : 32 mg/mL (108.73 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.3978 mL 16.9889 mL 33.9778 mL5 mM 0.6796 mL 3.3978 mL 6.7956 mL10 mM 0.3398 mL 1.6989 mL 3.3978 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL A

3、CTIVITY物活性 Puromycin aminonucleoside (NSC 3056)種氨 核苷類(lèi)抗素，為嘌呤霉素類(lèi)似物，于腎病動(dòng)物模型。體外研究Puromycin aminonucleoside (NSC 3056) (30 g/mL) markedly increases p53 protein levels in podocytes.1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEPuromycin aminonucleoside (NSC 3056)-induced podocyte apoptosis is p53 depen

4、dent and supports thenotion that dexamethasone exerts an antiapoptotic effect on cells that are exposed to Puromycinaminonucleoside (NSC 3056) through the downregulation of p53. Puromycin aminonucleoside (NSC 3056)induces podocyte apoptosis in a time-dependent manner 1. The IC50 values for PMAT-expr

5、essing andvector-transfected cells are 48.9 and 122.1 M, respectively, suggesting expression of PMAT-enhanced cellsensitivity to Puromycin aminonucleoside. Puromycin aminonucleoside (NSC 3056) (250 M) is toxic to bothPMAT-expressing and vector-transfected cells. Puromycin aminonucleoside (NSC 3056)

6、uptake in PMAT-expressing cells is fourfold higher at pH 6.6 than that at pH 7.4 2.體內(nèi)研究 The number of podocytes per glomerulus is 95.517.6 in the control rats, 90.7 on Day 4 in Puromycinaminonucleoside (NSC 3056) (8 mg/100 g, i.v.)-treated nephrosis rats. The amount of nephrin perglomerulus in contr

7、ol rats is 1.020.11 fmol and those in Puromycin aminonucleoside (NSC 3056) nephrosisrats are reduced to 0.460.06 fmol and 0.350.04 fmol on Day 4 and Day 7. The nephrin amount perpodocyte is significantly decreased association with the development of proteinuria in Puromycinaminonucleoside (NSC 3056)

8、 nephrosis rats 3. Rats given Puromycin aminonucleoside (NSC 3056) (100mg/kg, s.c.) gain less weight and their serum creatinine levels are higher than the control rats 4.PROTOCOLCell Assay 2 Cells are seeded in MEM with 10% FBS on 96-well plates at a density of 5,000 cells/well. After appr 48-hincub

9、ation (appr 40-50% confluence), cells are changed to fresh growth medium containing Puromycinaminonucleoside (NSC 3056) at various concentrations. For the protection experiment, cells are incubated inmedium containing 250 M Puromycin aminonucleoside (NSC 3056) with or without the PMAT inhibitordecyn

10、ium-22 (2 M). After a total of 72-h incubation in a 95% O2 incubator at 37C, cells are washed and theplates. The IC50 values are determined by fitting the cell growth data to the following model using nonlinearregression (WinNonLin version 3.2): S=Smax Smax S0 C/(C + IC50), where S is the cell survi

11、valexpressed as percentage of the optical density to untreated control cells, Smax is the maximal cell survival,S0 is the lowest residual cell survival at the high drug concentration, C is Puromycin aminonucleosideconcentration, is the Hill coefficient, and IC50 is the Puromycin aminonucleoside conc

12、entration leading tohalf-maximal cell survival. Five to six determinations are carried out within each experiment, and fourindependent experiments are performed.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Male F344 rats at 11 weeks of age are

13、 purchased from JaPuromycin aminonucleoside SLC. Normal rats andAdministration 3 a Puromycin aminonucleoside nephrosis model are used in the present study. Puromycin aminonucleoside(NSC 3056) nephrosis is induced in rats by a single intravenous injection of Puromycin aminonucleoside at adose of 8 mg

14、/100 g body weight in saline. Control animals receive an identical volume of saline. Nephroticrats (n=6 per group) are studied at Days 4 and 7 after the Puromycin aminonucleoside injection.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Ma

15、ster of Small Molecules 您邊的抑制劑師www.MedChemE1. Wada T, et al. Dexamethasone prevents podocyte apoptosis induced by puromycin aminonucleoside: role of p53 and Bcl-2-relatedfamily proteins. J Am Soc Nephrol. 2005 Sep;16(9):2615-25.2. Xia L, et al. Podocyte-specific expression of organic cation transpor

16、ter PMAT: implication in puromycin aminonucleosidenephrotoxicity.Am J Physiol Renal Physiol. 2009 Jun;296(6):F1307-13.3. Kawakami H, et al. Dynamics of absolute amount of nephrin in a single podocyte in puromycin aminonucleoside nephrosis ratscalculated by quantitative glomerular proteomics approach with selected reaction monitoring mode. Nephrol Dial Transplant. 2012 Apr;4. Nosaka K, et al. An adenosine deaminase inhibitor prevents puromycin aminonucleoside nephrotoxicity. Free Radic Biol Med 1997 ;22(4): 597-605.5. Furness PN, et al. An evaluation of experimental models of glo