| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
| Targets |
The primary target of Trabodenoson is the adenosine A1 receptor, a G protein-coupled receptor that is widely expressed in the heart, brain, and other tissues. By activating the A1 receptor, trabodenoson reduces heart rate, prolongs the atrioventricular (AV) nodal conduction time, and protects the heart against ischemia-reperfusion injury. These effects make it a potential therapeutic agent for atrial fibrillation and heart failure.
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| ln Vitro |
Trabodenson administration decreased the expression of type IV collagen and fibronectin while dramatically increasing S MMP-2 activity and MMP-14 abundance [1].
In vitro, trabodenoson has been shown to be a potent and selective agonist of the adenosine A1 receptor. It activates A1 receptor-mediated signaling pathways, including the inhibition of adenylyl cyclase and the activation of G protein-coupled inwardly rectifying potassium (GIRK) channels. The compound's selectivity for A1 over other adenosine receptors has been confirmed. |
| ln Vivo |
Trabodenson (6.0%), demonstrating a mean IOP reduction in juvenile rats over a 7-day period of 2.45 ± 0.38 mm Hg (downregulation) [1]. When compared to vehicle-treated non-induced eyes, topical Trabodenson dramatically increased nestin expression in ONH of induced eyes [2]. When compared to eyes treated with a vehicle, telabodisone-treated eyes showed a considerable reduction in optic nerve (ON) edema. In eyes treated with Trabodeson as opposed to eyes treated with vehicle, RGC counts were greater (74% in fellow eyes versus 47% in fellow eyes) [2].
In vivo, trabodenoson has been studied for its cardiovascular effects. It reduces heart rate and prolongs the PR interval in animal models. The compound has been investigated in clinical trials for the treatment of atrial fibrillation and heart failure. It is administered orally and is generally well-tolerated. |
| Enzyme Assay |
In vitro enzyme or receptor binding assays for trabodenoson involve studying its binding affinity for the adenosine A1 receptor. Radioligand binding assays are performed using membrane preparations from cells expressing the A1 receptor. The compound is incubated with a radiolabeled ligand, such as [3H]DPCPX, and the displacement of the ligand is measured to determine the affinity. Selectivity is assessed by testing the compound against other adenosine receptors.
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| Cell Assay |
In vitro cell-based assays for trabodenoson are performed using cells that express the A1 receptor. Cells are treated with the compound, and the inhibition of cAMP production is measured as a functional readout of A1 receptor activation. The compound's effects on GIRK channel activation are assessed using electrophysiological techniques.
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| Animal Protocol |
Animal/Disease Models: young (3-4 months old) and old (12 months old) [1].
Doses: 3% or 6% in 10 μL. Route of Administration: Eye drops for 7 days Experimental Results: Intraocular pressure decreases. In vivo animal experiments for trabodenoson are conducted using rodent and canine models of cardiovascular disease. The compound is administered orally or intravenously, and heart rate, blood pressure, and ECG parameters are measured. The compound's effects on atrial fibrillation and ischemia-reperfusion injury are assessed. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of trabodenoson indicate that it is orally active. The compound has a molecular weight of 377.44 and a molecular formula of C19H23N5O4. It is a solid at room temperature. Specific PK parameters, such as half-life and bioavailability, are determined in clinical studies via LC-MS/MS analysis of plasma samples. The compound is metabolized in the liver and excreted renally.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for trabodenoson indicate that it is generally well-tolerated. Common side effects may include headache, dizziness, and nausea. The compound may also cause bradycardia and hypotension due to its effects on the cardiovascular system. It should be used with caution in patients with pre-existing cardiovascular conditions.
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| References |
[1]. Guorong Li, et al. Trabodenoson, an Adenosine Mimetic With A1 Receptor Selectivity Lowers Intraocular Pressure by Increasing Conventional Outflow Facility in Mice. Invest Ophthalmol Vis Sci. 2018 Jan 1;59(1):383-392.
[2]. Yan Guo, et al. Topical Trabodenoson Is Neuroprotective in a Rodent Model of Anterior Ischemic Optic Neuropathy (rNAION). Transl Vis Sci Technol. 2019 Dec 20;8(6):47. |
| Additional Infomation |
Tribodinosone has been used in trials investigating the treatment of ocular hypertension (OHT) and primary open-angle glaucoma (POAG).
Other information: Trabodenoson is an adenosine A1 receptor agonist. It is also known as INNO8875 and PJ875. The compound has been investigated for the treatment of atrial fibrillation and heart failure. Its CAS number is 871108-05-3. |
| Molecular Formula |
C15H20N6O6
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| Molecular Weight |
380.356
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| Exact Mass |
380.144
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| CAS # |
871108-05-3
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| PubChem CID |
11610599
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| Appearance |
White to yellow solid powder
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| Density |
1.9±0.1 g/cm3
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| Boiling Point |
691.2±65.0 °C at 760 mmHg
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| Flash Point |
371.8±34.3 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.816
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| LogP |
2.61
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
531
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O[C@@H]1[C@H](O)[C@@H](CO[N+](=O)[O-])O[C@H]1N1C=NC2C(=NC=NC1=2)NC1CCCC1
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| InChi Key |
AQLVRTWKJDTWQQ-SDBHATRESA-N
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| InChi Code |
InChI=1S/C15H20N6O6/c22-11-9(5-26-21(24)25)27-15(12(11)23)20-7-18-10-13(16-6-17-14(10)20)19-8-3-1-2-4-8/h6-9,11-12,15,22-23H,1-5H2,(H,16,17,19)/t9-,11-,12-,15-/m1/s1
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| Chemical Name |
[(2R,3S,4R,5R)-5-[6-(cyclopentylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl nitrate
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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 (~328.64 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.47 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 (5.47 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 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 (5.47 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 | 2.6291 mL | 13.1454 mL | 26.2909 mL | |
| 5 mM | 0.5258 mL | 2.6291 mL | 5.2582 mL | |
| 10 mM | 0.2629 mL | 1.3145 mL | 2.6291 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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