| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
A3 adenosine receptor ( Ki = 0.33 nM )
A3 adenosine receptor (A3AR). Namodenoson is a selective A3AR agonist with a Ki of 0.33 nM. It displays 2500- and 1400-fold selectivity over A1 and A2A receptors, respectively. Namodenoson is a selective A3 adenosine receptor (A3AR) agonist. |
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| ln Vitro |
Namodenoson (2-Cl-IB-MECA) 100 nM significantly reorganized the cytoskeleton in human ADF cells of the astroglial lineage, resulting in the appearance of stress fibers and multiple cell protrusions. High Namodenoson (2-Cl-IB-MECA) concentrations directly result in a Ca2+ influx[2].
Namodenoson is a high-affinity, selective agonist for the A3 adenosine receptor. It has shown promise in the treatment of NASH by modulating the PI3K/NF-κB/Wnt/β-catenin signaling pathway. Namodenoson has shown promise in the treatment of non-alcoholic steatohepatitis (NASH) by exerting its effects through the dysregulation of the PI3K/NF-κB/Wnt/β-catenin signaling pathway. |
| ln Vivo |
After receiving 200 μg/kg of Namodenoson (2-Cl-IB-MECA) intravenously, there was a brief drop in blood pressure and a 50–100 fold increase in plasma histamine levels. Hemodynamic effects were absent when Namodenoson (2-Cl-IB-MECA) was administered in two doses[1].
Namodenoson has shown promise in the treatment of non-alcoholic steatohepatitis (NASH). Its in vivo efficacy has been studied in preclinical models and clinical trials for NASH and liver cancer. Namodenoson has shown promise in the treatment of non-alcoholic steatohepatitis (NASH). |
| Enzyme Assay |
Specific protocols for in vitro receptor binding assays for Namodenoson are not detailed. Its activity is assessed using radioligand binding assays to measure its affinity for A3, A1, and A2A adenosine receptors. Namodenoson is a selective A3AR agonist with a Ki of 0.33 nM.
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| Cell Assay |
The indicated drug concentrations were applied to the cells for a duration of 48 hours.
Cellular assays for Namodenoson involve treating cells expressing adenosine receptors with the compound and measuring receptor activation and downstream signaling. Its effects on the PI3K/NF-κB/Wnt/β-catenin pathways can be assessed. Namodenoson has shown promise in the treatment of NASH by modulating the PI3K/NF-κB/Wnt/β-catenin signaling pathway. |
| Animal Protocol |
In vivo animal model protocols for Namodenoson involve its administration to animal models of NASH and liver cancer to study its efficacy. Namodenoson has shown promise in the treatment of non-alcoholic steatohepatitis (NASH).
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Namodenoson is not available in the provided references. As an orally active compound, its PK properties would be evaluated in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Namodenoson is not available in the provided references. As an investigational drug, its safety profile is being evaluated in clinical trials.
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| References | |
| Additional Infomation |
Namodinosin has been used in clinical trials for the treatment of chronic hepatitis C and hepatocellular carcinoma. Namodinosin is a highly bioavailable, synthetic, selective adenosine A3 receptor (A3AR) agonist with potential antitumor activity. Namodinosin selectively binds to and activates A3AR expressed on the cell surface, thereby inhibiting downstream Wnt and NF-κB signaling pathways, potentially leading to apoptosis in A3AR-expressing tumor cells. A3AR is a G protein-coupled receptor highly expressed on the surface of various solid tumor cells, including hepatocellular carcinoma (HCC) cells, and plays an important role in cell proliferation.
Namodenoson is an investigational drug being developed for the treatment of NASH and liver cancer. It is a selective A3 adenosine receptor agonist. Namodenoson (2 Cl-IB-MECA; CF102) (CAS#: 163042-96-4) is a selective A3 adenosine receptor (A3AR) agonist. |
| Molecular Formula |
C18H18CLIN6O4
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|---|---|
| Molecular Weight |
544.7308
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| Exact Mass |
544.012
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| Elemental Analysis |
C, 39.69; H, 3.33; Cl, 6.51; I, 23.30; N, 15.43; O, 11.75
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| CAS # |
163042-96-4
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| PubChem CID |
3035850
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| Appearance |
Solid powder
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| Density |
2.0±0.1 g/cm3
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| Melting Point |
209 °C
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| Index of Refraction |
1.814
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| LogP |
3.14
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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 |
5
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| Heavy Atom Count |
30
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| Complexity |
623
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| Defined Atom Stereocenter Count |
4
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| SMILES |
IC1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])N([H])C1=C2C(=NC(=N1)Cl)N(C([H])=N2)[C@@]1([H])[C@@]([H])([C@@]([H])([C@@]([H])(C(N([H])C([H])([H])[H])=O)O1)O[H])O[H]
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| InChi Key |
IPSYPUKKXMNCNQ-PFHKOEEOSA-N
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| InChi Code |
InChI=1S/C18H18ClIN6O4/c1-21-16(29)13-11(27)12(28)17(30-13)26-7-23-10-14(24-18(19)25-15(10)26)22-6-8-3-2-4-9(20)5-8/h2-5,7,11-13,17,27-28H,6H2,1H3,(H,21,29)(H,22,24,25)/t11-,12+,13-,17+/m0/s1
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| Chemical Name |
(2S,3S,4R,5R)-5-[2-chloro-6-[(3-iodophenyl)methylamino]purin-9-yl]-3,4-dihydroxy-N-methyloxolane-2-carboxamide
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| Synonyms |
CF102; Cl-IB-MECA; CF-102; 2-Cl-IB-MECA; CF 102; Namodenoson; Chloro-IB-MECA
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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: ~100 mg/mL (~183.6 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.82 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. Solubility in Formulation 2: 2.08 mg/mL (3.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 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: ≥ 2.08 mg/mL (3.82 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 | 1.8358 mL | 9.1789 mL | 18.3577 mL | |
| 5 mM | 0.3672 mL | 1.8358 mL | 3.6715 mL | |
| 10 mM | 0.1836 mL | 0.9179 mL | 1.8358 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04697810 | Recruiting | Drug: Namodenoson Drug: Placebo |
NASH - Nonalcoholic Steatohepatitis |
Can-Fite BioPharma | December 10, 2021 | Phase 2 |
| NCT05201404 | Recruiting | Drug: Namodenoson Drug: Placebo |
Hepatocellular Carcinoma Cirrhosis |
Can-Fite BioPharma | March 15, 2023 | Phase 3 |
| NCT02927314 | Completed | Drug: CF102 Drug: Placebo |
Non-alcoholic Steatohepatitis (NASH) |
Can-Fite BioPharma | November 27, 2017 | Phase 2 |
| NCT00790673 | Completed | Drug: CF102 Drug: Placebo |
Chronic Hepatitis C | Can-Fite BioPharma | July 2009 | Phase 1 Phase 2 |
| NCT00790218 | Completed | Drug: CF102 | Hepatocellular Carcinoma | Can-Fite BioPharma | February 2009 | Phase 1 Phase 2 |
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