| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
Adenylyl cyclase (IC50 = 3 µM)[1]
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| ln Vitro |
2',5'-Dideoxyadenosine (10 μM, 30 minutes) inhibits the phosphorylation of GluA1 at Ser845 caused by carbachol (CCh) and decreases the generation of cAMP [3]. In 30 minutes, 10 μM 2',5'-Dideoxyadenosine phosphorylates Akt and disconnects Ser2448 phosphorylation produced by CCh [3]. The inotropic and chronotropic effects of isopropanol (8-54 pmol) β-hexanosine are substantially and reversibly blocked by 2',5'-Dideoxyadenosine (20-150 mM), just like adenosine does. up to 50% and 70%, in that order [2].
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| ln Vivo |
In this study the effects of 2',5'-dideoxyadenosine (DDA), an agonist of the intracellular adenosine binding site (P-site), on myocardial contractility, coronary resistance and cAMP-metabolism in the isolated guinea-pig heart were compared with those of adenosine. DDA (20-150 microM), like adenosine, dose dependently and reversibly inhibited the positive inotropic and chronotropic effect of beta-adrenergic stimulation with isoproterenol (8-54 pmol) up to 70% and 50%, respectively. In contrast to the known vasodilatory action of adenosine, however, basal coronary resistance remained unchanged with DDA. The antiadrenergic action of DDA was parallelled by changes in cAMP release from heart: stimulation with isoproterenol (16 pmol) increased cAMP release from 1.5 +/- 0.14 pmol cAMP/min under basal conditions to 5.2 +/- 0.45 pmol/min (mean +/- SE; n = 4). This increase was inhibited by 49% in presence of DDA (90 microM). Theophylline (50 microM), a well known antagonist of extracellular adenosine receptors, did not alter the potency of DDA. Our findings demonstrate, that DDA does not alter basal coronary flow but exerts a potent antiadrenergic action in heart which is P-site mediated[2].
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| Enzyme Assay |
M1 muscarinic acetylcholine receptors are highly expressed in key areas that control cognition, such as the cortex and hippocampus, representing one potential therapeutic target for cognitive dysfunctions of Alzheimer's disease and schizophrenia. We have reported that M1 receptors facilitate cognition by promoting membrane insertion of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor AMPA receptor subunit 1 (GluA1) through phosphorylation at Ser845. However, the signaling pathway is still unclear. Here we showed that adenylyl cyclase inhibitor 2',5'-dideoxyadenosine and PKA inhibitor KT5720 inhibited enhancement of phosphorylation of Ser845 and membrane insertion of GluA1 induced by M1 receptor activation. Furthermore, PI3K inhibitor LY294002 and protein kinase B (Akt) inhibitor IV blocked the effects of M1 receptors as well. Remarkably, the increase of the activity of PI3K-Akt signaling induced by M1 receptor activation could be abolished by cAMP-PKA inhibitors. Moreover, inhibiting the mammalian target of rapamycin (mTOR) complex 1, an important downstream effector of PI3K-Akt, by short-term application of rapamycin attenuated the effects of M1 receptors on GluA1. Furthermore, such effect was unrelated to possible protein synthesis promoted by mTOR. Taken together, these data demonstrate that M1 receptor activation induces membrane insertion of GluA1 via a signaling linking cAMP-PKA and PI3K-Akt-mTOR pathways but is irrelevant to protein synthesis.-Zhao, L.-X., Ge, Y.-H., Li, J.-B., Xiong, C.-H., Law, P.-Y., Xu, J.-R., Qiu, Y., Chen, H.-Z. M1 muscarinic receptors regulate the phosphorylation of AMPA receptor subunit GluA1 via a signaling pathway linking cAMP-PKA and PI3K-Akt[3].
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| Cell Assay |
Western Blot Analysis [3]
Cell Types: Primary hippocampal neurons Tested Concentrations: 10 μM Incubation Duration: 30 minutes Experimental Results: Reduce cAMP production and block GluA1 Ser845 phosphorylation induced by carbachol (CCh). |
| Animal Protocol |
Animal/Disease Models: Male Wistar rats (3-4 months old) [3] 2',5'-dideoxyadenosine (0.1 mg/kg; intraperitoneal (ip) injection; sham for 15 minutes) completely inhibits Fr?EtOAc in suspension [4 ].
Doses: 0.1 mg/kg Route of Administration: IP; pretreatment for 15 minutes. Experimental Results: Completely inhibited the diuretic, natriuretic and K+ and Cl- preserving effects of Fr•EtOAc on rats. |
| References |
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| Additional Infomation |
2',5'-Dideoxyadenosine is a deoxyribonucleoside.
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| Molecular Formula |
C₁₀H₁₃N₅O₂
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|---|---|
| Molecular Weight |
235.24
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| Exact Mass |
235.107
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| CAS # |
6698-26-6
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| PubChem CID |
65166
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| Appearance |
Typically exists as White to off-white solids at room temperature
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| Density |
1.77 g/cm3
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| Boiling Point |
547ºC at 760 mmHg
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| Flash Point |
284.6ºC
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| Index of Refraction |
1.825
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| LogP |
0.658
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
292
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C[C@H]1O[C@H](C[C@@H]1O)N1C=NC2=C1N=CN=C2N
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| InChi Key |
FFHPXOJTVQDVMO-DSYKOEDSSA-N
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| InChi Code |
InChI=1S/C10H13N5O2/c1-5-6(16)2-7(17-5)15-4-14-8-9(11)12-3-13-10(8)15/h3-7,16H,2H2,1H3,(H2,11,12,13)/t5-,6+,7-/m1/s1
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| Chemical Name |
(2R,3S,5R)-5-(6-aminopurin-9-yl)-2-methyloxolan-3-ol
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| Synonyms |
2',5'Dideoxyadenosine; 2',5'-Dideoxyadenosine; 6698-26-6; (2R,3S,5R)-5-(6-Amino-9H-purin-9-yl)-2-methyltetrahydrofuran-3-ol; Adenosine, 2',5'-dideoxy-; 988H339Z1L; Adenosine,2',5'-dideoxy-; 5-(6-AMINOPURIN-9-YL)-2-METHYLTETRAHYDROFURAN-3-OL; NSC-95943; 2',5' Dideoxyadenosine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~531.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.63 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2510 mL | 21.2549 mL | 42.5098 mL | |
| 5 mM | 0.8502 mL | 4.2510 mL | 8.5020 mL | |
| 10 mM | 0.4251 mL | 2.1255 mL | 4.2510 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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