2-5-Dideoxyadenosine-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE2,5-DideoxyadenosineCat. No.: HY-135878CAS No.: 6698-26-6分式: CHNO分量: 235.24作靶点: Adenylate Cyclase; Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性数据体外实验 DMSO : 125 mg/mL (531.37 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.2510 mL 21.2549 mL 42.5098 mL5 mM 0.8502 mL 4.2510 mL 8.5020 mL10 mM 0.4251 mL 2.1255 mL 4.2510 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，配制前请先配制澄的储备液，再依次添加助溶剂(为保

3、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；澄的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: 2.08 mg/mL (8.84 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (8.84 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small

4、Molecules 您边的抑制剂师www.MedChemE物活性 2,5-Dideoxyadenosine种有效且竞争性的腺苷酸环化酶 (adenylyl cyclase) 抑制剂，可以有效结合 P位点，IC50 为 3 M。2,5-Dideoxyadenosine核苷类似物，在脏中发挥强的抗肾上腺素 (antiadrenergic) 作。IC50 & Target IC50: 3 M (adenylyl cyclase) 1体外研究 2,5-Dideoxyadenosine (10 M, 30 min) reduces cAMP production and blocks the phosp

5、horylation of GluA1at Ser845 induced by carbachol (CCh) 3.2,5-Dideoxyadenosine (10 M, 30 min) blocks CCh-induced increase of phosphorylation of Akt andattenuates CCh-induced phosphorylation of Ser2448 3.2,5-Dideoxyadenosine (20-150 mM), like adenosine, dependently and reversibly inhibits the positiv

6、einotropic and chronotropic effect of beta-adrenergic stimulation with isoproterenol (8-54 pmol) up to 70% and50%, respectively 2.Western Blot Analysis 3Cell Line: Primary hippocampal neuronsConcentration: 10 MIncubation Time: 30 minResult: Reduced cAMP production and blocked the phosphorylation of

7、GluA1 at Ser845 inducedby carbachol (CCh).体内研究 2,5-Dideoxyadenosine (0.1 mg/kg; IP; 15 min pre-treated) fully inhibits the diuretic, natriuretic and K+ andCl- sparing effect of FrEtOAc in rats 4.Animal Model: Male Wistar rats (3-4 months old) 3Dosage: 0.1 mg/kgAdministration: IP; 15 min pre-treatedR

8、esult: Fully inhibited the diuretic, natriuretic and K+ and Cl- sparing effect of FrEtOAc in rats.REFERENCES1. Bushfield M, et al. Tissue levels, source, and regulation of 3-AMP: an intracellular inhibitor of adenylyl cyclases. Mol Pharmacol. 1990Dec;38(6):848-53.2. Hartmann M, et al. Isoproterenol

9、antagonistic effect of 2,5-dideoxyadenosine in the isolated perfused guinea-pig heart. J Mol CellCardiol. 1993 Mar;25(3):331-8.3. Zhao LX, et al. M1 muscarinic receptors regulate the phosphorylation of AMPA receptor subunit GluA1 via a signaling pathway linkingcAMP-PKA and PI3K-Akt. FASEB J. 2019 Ma

10、y;33(5):6622-6631.4. Leme Tdos S, et al. Role of prostaglandin/cAMP pathway in the diuretic and hypotensive effects of purified fraction of Maytenus ilicifolia2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMart ex Reissek (Celastraceae). J Ethnopharmacol. 2013 Oct 28;150(1):154-61.McePdfHeightCaution: Product has not been fully valid