2-Hexynyl-5′-N-ethylcarboxamidoadenosine
Based on 1 Customer Validation
2-Hexynyl-5′-N-ethylcarboxamidoadenosine (HENECA) is a selective A2A adenosine receptor agonist. 2-Hexynyl-5′-N-ethylcarboxamidoadenosine increases intracellular cAMP level, and inhibits TNFα-evoked MMP-3 release. 2-Hexynyl-5′-N-ethylcarboxamidoadenosine induces Aβ42 production in SH-SY5Y cells.
For research use only. We do not sell to patients.
- Purity : 99.39%
- CAS No.: 141018-30-6
- Formula: C18H24N6O4
- Molecular Weight:388.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Adenosine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
A2AR |
Chemical Information
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CAS No. 141018-30-6
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Appearance Solid
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Molecular Weight 388.42
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Formula C18H24N6O4
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Color Off-white to pink
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SMILES
O[C@H]([C@@H]1O)[C@](O[C@@H]1C(NCC)=O)([H])N2C3=NC(C#CCCCC)=NC(N)=C3N=C2
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Synonyms
HENECA; 2-Hexynyl-NECA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 102 mg/mL (262.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.55 mg/mL (6.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.55 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.55 mg/mL (6.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.55 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Mitochondrial membrane-potential fluorescent assay
Mitochondrial membrane potential fluorescent assays estimate ΔΨm in living cells using lipophilic cationic dyes such as TMRM, TMRE, rhodamine 123, and JC-1, which accumulate in mitochondria according to membrane polarization; loss of signal after FCCP or CCCP treatment is interpreted as mitochondrial depolarization. TMRM/TMRE and rhodamine 123 are commonly used for semi-quantitative live-cell microscopy or flow cytometry, while JC-1 can report a shift from red aggregate fluorescence to green monomer fluorescence during depolarization; interpretation requires controls because dye concentration, quenching mode, cell type, dye efflux, and mitochondrial mass can affect fluorescence independently of ΔΨm.
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Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
Purity & Documentation
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Cunha RA, et al. ZM241385 is an antagonist of the facilitatory responses produced by the A2A adenosine receptor agonists CGS21680 and HENECA in the rat hippocampus. Br J Pharmacol. 1997 Dec;122(7):1279-84. [Content Brief]
[2]. Konishi H, et al. Adenosine inhibits TNFα-induced MMP-3 production in MH7A rheumatoid arthritis synoviocytes via A2A receptor signaling. Sci Rep. 2022 Apr 11;12(1):6033 [Content Brief]
[3]. Nagpure BV, et al. Hydrogen sulfide inhibits A2A adenosine receptor agonist induced β-amyloid production in SH-SY5Y neuroblastoma cells via a cAMP dependent pathway. PLoS One. 2014 Feb 11;9(2):e88508. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5745 mL | 12.8727 mL | 25.7453 mL | 64.3633 mL |
| 5 mM | 0.5149 mL | 2.5745 mL | 5.1491 mL | 12.8727 mL | |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5745 mL | 6.4363 mL | |
| 15 mM | 0.1716 mL | 0.8582 mL | 1.7164 mL | 4.2909 mL | |
| 20 mM | 0.1287 mL | 0.6436 mL | 1.2873 mL | 3.2182 mL | |
| 25 mM | 0.1030 mL | 0.5149 mL | 1.0298 mL | 2.5745 mL | |
| 30 mM | 0.0858 mL | 0.4291 mL | 0.8582 mL | 2.1454 mL | |
| 40 mM | 0.0644 mL | 0.3218 mL | 0.6436 mL | 1.6091 mL | |
| 50 mM | 0.0515 mL | 0.2575 mL | 0.5149 mL | 1.2873 mL | |
| 60 mM | 0.0429 mL | 0.2145 mL | 0.4291 mL | 1.0727 mL | |
| 80 mM | 0.0322 mL | 0.1609 mL | 0.3218 mL | 0.8045 mL | |
| 100 mM | 0.0257 mL | 0.1287 mL | 0.2575 mL | 0.6436 mL |
2-Hexynyl-5′-N-ethylcarboxamidoadenosine Related Classifications
HY-137370 Related Classifications
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