| Bioactivity | 2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart[1][2]. | ||||||||||||
| Target | IC50: 3 µM (adenylyl cyclase) | ||||||||||||
| Invitro | 2',5'-Dideoxyadenosine (10 μM, 30 min) reduces cAMP production and blocks the phosphorylation of GluA1 at Ser845 induced by carbachol (CCh)[3]. 2',5'-Dideoxyadenosine (10 μM, 30 min) blocks CCh-induced increase of phosphorylation of Akt and attenuates CCh-induced phosphorylation of Ser2448[3]. 2',5'-Dideoxyadenosine (20-150 mM), like adenosine, dependently and reversibly inhibits the positive inotropic and chronotropic effect of beta-adrenergic stimulation with isoproterenol (8-54 pmol) up to 70% and 50%, respectively[2]. Western Blot Analysis[3] Cell Line: | ||||||||||||
| In Vivo | 2',5'-Dideoxyadenosine (0.1 mg/kg; IP; 15 min pre-treated) fully inhibits the diuretic, natriuretic and K+ and Cl- sparing effect of Fr•EtOAc in rats[4]. Animal Model: | ||||||||||||
| Name | 2',5'-Dideoxyadenosine | ||||||||||||
| CAS | 6698-26-6 | ||||||||||||
| Formula | C10H13N5O2 | ||||||||||||
| Molar Mass | 235.24 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Bushfield M, et al. Tissue levels, source, and regulation of 3'-AMP: an intracellular inhibitor of adenylyl cyclases. Mol Pharmacol. 1990 Dec;38(6):848-53. [2]. Hartmann M, et al. Isoproterenol antagonistic effect of 2',5'-dideoxyadenosine in the isolated perfused guinea-pig heart. J Mol Cell Cardiol. 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 linking cAMP-PKA and PI3K-Akt. FASEB J. 2019 May;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 ilicifolia Mart ex Reissek (Celastraceae). J Ethnopharmacol. 2013 Oct 28;150(1):154-61. |