Namodenoson
Based on 3 publication(s) in Google Scholar
Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.56%
- CAS. Nr.: 163042-96-4
- Formel: C18H18ClIN6O4
- Molecular Weight:544.73
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Namodenoson
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.2 nM
Compound: 2, CI-IB-MECA
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Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
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[PMID: 18255292] |
| CHO | IC50 |
1.21 nM
Compound: Cl-IB-MECA
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Agonist activity at human recombinant A3AR expressed in CHO cells assessed as inhibition of forskolin-induced stimulation of cAMP production
Agonist activity at human recombinant A3AR expressed in CHO cells assessed as inhibition of forskolin-induced stimulation of cAMP production
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[PMID: 24931275] |
| CHO | IC50 |
2.2 nM
Compound: Cl-IB-MECA
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Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
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[PMID: 15481989] |
| HEK293 | EC50 |
0.15 nM
Compound: 1b, CI-IB-MECA
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Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
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[PMID: 23789857] |
| HEK293 | EC50 |
0.46 nM
Compound: 55
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Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
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[PMID: 26890707] |
| HEK293 | EC50 |
4.1 nM
Compound: 38; Cl-IBMECA
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Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
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[PMID: 32271569] |
| HEK293 | ED50 |
100 nM
Compound: 2, Cl-IB-MECA
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Activity at adenosine A3 receptor expressed in HEK293 cells by inhibition of isoprotenol-stimulated cAMP gated channel
Activity at adenosine A3 receptor expressed in HEK293 cells by inhibition of isoprotenol-stimulated cAMP gated channel
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[PMID: 16487705] |
In human ADF cells of astroglial lineage, 100 nM Namodenoson (2-Cl-IB-MECA) caused a marked reorganization of the cytoskeleton, with appearance of stress fibres and numerous cell protrusions. High concentrations of Namodenoson (2-Cl-IB-MECA) directly cause influx of Ca2+[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 163042-96-4
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Appearance Solid
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Molecular Weight 544.73
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Formel C18H18ClIN6O4
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Color White to off-white
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SMILES
ClC1=NC(NCC2=CC=CC(I)=C2)=C3N=CN([C@@H]4O[C@H](C(NC)=O)[C@@H](O)[C@H]4O)C3=N1
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Synonyms
CF-102; 2-Cl-IB-MECA
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Br J Pharmacol
An adenosinergic positive feedback loop extends pharmacological cardioprotection duration. [Abstract]2024 Dec;181(23):4920-4936. PMID: 39256947 -
J Inflamm Res
Adenosine A2A Receptor Activation Alleviated Disease of Mice with Systemic Candida albicans Infection by Regulating Macrophage Function. [Abstract]2025 Mar 6:18:3283-3294. PMID: 40065909 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (183.58 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (3.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (3.82 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Van Schaick EA et al. Hemodynamic effects and histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats. Eur J Pharmacol. 1996 Jul 25;308(3):311-4. [Content Brief]
[2]. Jacobson KA et al. Adenosine A3 receptors: novel ligands and paradoxical effects. Trends Pharmacol Sci. 1998 May;19(5):184-91. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8358 mL | 9.1789 mL | 18.3577 mL | 45.8943 mL |
| 5 mM | 0.3672 mL | 1.8358 mL | 3.6715 mL | 9.1789 mL | |
| 10 mM | 0.1836 mL | 0.9179 mL | 1.8358 mL | 4.5894 mL | |
| 15 mM | 0.1224 mL | 0.6119 mL | 1.2238 mL | 3.0596 mL | |
| 20 mM | 0.0918 mL | 0.4589 mL | 0.9179 mL | 2.2947 mL | |
| 25 mM | 0.0734 mL | 0.3672 mL | 0.7343 mL | 1.8358 mL | |
| 30 mM | 0.0612 mL | 0.3060 mL | 0.6119 mL | 1.5298 mL | |
| 40 mM | 0.0459 mL | 0.2295 mL | 0.4589 mL | 1.1474 mL | |
| 50 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9179 mL | |
| 60 mM | 0.0306 mL | 0.1530 mL | 0.3060 mL | 0.7649 mL | |
| 80 mM | 0.0229 mL | 0.1147 mL | 0.2295 mL | 0.5737 mL | |
| 100 mM | 0.0184 mL | 0.0918 mL | 0.1836 mL | 0.4589 mL |
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