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NECA (5'-N-Ethylcarboxamidoadenosine) is a novel and potent adenosine receptor agonist with Ki values of 6.2, 14, and 20 nM for human A3, A1 and A2A receptors, respectively, and an EC50 of 2.4 μM for human A2B. It can prevent platelet aggregation and is centrally active in vivo.
| Targets |
Adenosine receptor; IL-18; TNF-α; CD54; JNK
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|---|---|
| ln Vitro |
5'-N-Ethylcarboxamidoadenosine (NECA) administration results in a dose-dependent significant decrease in the mean number of cocaine infusions obtained per session [5'-N-Ethylcarboxamidoadenosine (NECA): F(4,12)=14.9; P<0.001]. Significantly higher latencies than those obtained for vehicle treatment are observed upon administration of 5'-N-Ethylcarboxamidoadenosine (NECA) [F(4,12)=16.1; P<0.001][1]. In diabetic rats, daily intraperitoneal injections of 5'-N-Ethylcarboxamidoadenosine (NECA) at 0.3 mg/kg/day for two weeks lower MDA levels; control rats do not experience this same reduction. In diabetic rats, daily administration of NECA (0.3 mg/kg/day, i.p.) for two weeks decreases the gene expression of TNF-α and interleukin (IL)-18 induced by diabetes, while having no effect on control rats. For two weeks, a daily intraperitoneal injection of 5'-N-Ethylcarboxamidoadenosine (NECA) at a dose of 0.3 mg/kg/day inhibits the activation of JNK MAPK in diabetic rats, while having no effect on control rats[2].
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| ln Vivo |
The mean number of cocaine infusions per injection was significantly reduced in a dose-dependent manner after administration of 5'-N-ethylcarboxamideadenosine (NECA) [5'-N-ethylcarboxamideadenosine (NECA): F(4,12)= 14.9; P<0.001]. Administration of 5'-N-ethylcarboxamide adenosine (NECA) [F(4,12)=16.1; P<0.001] resulted in a significant increase in latency above the values obtained with vehicle treatment [1]. Daily intraperitoneal injection of 5'-N-ethylcarboxamide adenosine (NECA) at a dose of 0.3 mg/kg/day for two weeks reduced malondialdehyde (MDA) levels in diabetic rats but did not affect controls rat. Daily treatment with NECA (0.3 mg/kg/day, intraperitoneally for two weeks) reduced diabetes-induced gene expression of tumor necrosis factor (TNF)-α and interleukin (IL)-18 in diabetic rats, but not Affected control rats. Daily intraperitoneal injection of 5'-N-ethylcarboxamide adenosine (NECA) 0.3 mg/kg/day for two weeks also blocked the activation of JNK MAPK in diabetic rats but did not affect control rats [2 ].
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| Animal Protocol |
For this experiment, male Wistar rats are utilized. The weight of these animals varies from 350 to 425 g. They live in separate hanging wire cages with a 12-hour light/dark cycle. Four rats are used to test the effects of 5'-N-Ethylcarboxamidoadenosine (NECA). 15 minutes before the start of the test sessions, either 5'-N-Ethylcarboxamidoadenosine (NECA) (5, 7.5, 10, 20 μg/kg) or vehicle (saline) is given intraperitoneally. A random order crossover design is used in the administration of 5'-N-Ethylcarboxamidoadenosine (NECA). Animals are tested twice with the same dosage in the majority of cases[1].
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| References | |
| Additional Infomation |
N-ethyl-5'-carboxamidoadenosine is a derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group. It has a role as an adenosine A1 receptor agonist, an adenosine A2A receptor agonist, an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor, an antineoplastic agent and a vasodilator agent. It is a member of adenosines and a monocarboxylic acid amide. It is functionally related to an adenosine.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. |
| Molecular Formula |
C12H16N6O4
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|---|---|
| Molecular Weight |
308.29324
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| Exact Mass |
308.123
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| CAS # |
35920-39-9
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| PubChem CID |
448222
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| Appearance |
White to off-white solid powder
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| Density |
1.9±0.1 g/cm3
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| Melting Point |
229-231ºC
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| Index of Refraction |
1.829
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| LogP |
-0.48
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
426
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O[C@H]1[C@H](N2C=NC3=C(N)N=CN=C23)O[C@H](C(NCC)=O)[C@H]1O
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| InChi Key |
JADDQZYHOWSFJD-FLNNQWSLSA-N
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| InChi Code |
InChI=1S/C12H16N6O4/c1-2-14-11(21)8-6(19)7(20)12(22-8)18-4-17-5-9(13)15-3-16-10(5)18/h3-4,6-8,12,19-20H,2H2,1H3,(H,14,21)(H2,13,15,16)/t6-,7+,8-,12+/m0/s1
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| Chemical Name |
(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-N-ethyl-3,4-dihydroxyoxolane-2-carboxamide
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| Synonyms |
5'-N-Ethylcarboxamidoadenosine; NECA
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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: 62~62.5 mg/mL (201.1~202.7 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.11 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.11 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.11 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 | 3.2437 mL | 16.2185 mL | 32.4370 mL | |
| 5 mM | 0.6487 mL | 3.2437 mL | 6.4874 mL | |
| 10 mM | 0.3244 mL | 1.6218 mL | 3.2437 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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