2-5-Dideoxyadenosine-DataSheet-生命科學試劑-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作靶點: Adenylate Cyclase; Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (531.37 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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?，配制前請先配制澄的儲備液，再依次添加助溶?為保

3、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；澄的儲備液可以根據(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: 2.08 mg/mL (8.84 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (8.84 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small

4、Molecules 您邊的抑制劑師www.MedChemE物活性 2,5-Dideoxyadenosine種有效且競爭性的腺苷酸環(huán)化酶 (adenylyl cyclase) 抑制劑，可以有效結(jié)合 P位點，IC50 為 3 M。2,5-Dideoxyadenosine核苷類似物，在臟中發(fā)揮強的抗腎上腺素 (antiadrenergic) 作。IC50 & Target IC50: 3 M (adenylyl cyclase) 1體外研究 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).體內(nèi)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 您邊的抑制劑師www.MedChemEMart ex Reissek (Celastraceae). J Ethnopharmacol. 2013 Oct 28;150(1):154-61.McePdfHeightCaution: Product has not been fully valid