| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Other Sizes |
| Targets |
ANR-94 targets the adenosine A2A receptor (AA2AR), a G protein-coupled receptor that is widely expressed in the brain, particularly in the striatum. AA2AR plays a critical role in modulating neurotransmitter release and motor function. Antagonism of AA2AR has been shown to have neuroprotective effects and is a promising therapeutic strategy for Parkinson's disease. By selectively blocking AA2AR, ANR-94 modulates dopaminergic signaling and may reduce motor symptoms in Parkinson's disease. Its potent and selective inhibition of hAA2AR (Ki = 46 nM) makes it a valuable tool for studying AA2AR biology and for developing Parkinson's disease therapeutics.
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| ln Vitro |
In vitro, ANR-94 demonstrates potent antagonism of the adenosine A2A receptor with a Ki of 46 nM for hAA2AR. The compound's activity is concentration-dependent, with effective concentrations in the nanomolar range. In cell-based assays, ANR-94 inhibits AA2AR-mediated signaling, as measured by reduced cAMP production. It also exhibits antiviral activity against SARS-CoV-2, inhibiting SARS-CoV-2-induced cytotoxicity in Caco-2 cells and VERO-6 cells at 10 µM after 48 hours. Its potent AA2AR antagonism and antiviral activity make it a valuable tool for studying AA2AR function and viral infection.
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| ln Vivo |
In vivo, ANR-94 has been studied in preclinical models of Parkinson's disease. Its ability to antagonize AA2AR and modulate dopaminergic signaling may lead to neuroprotective effects and improved motor function. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying AA2AR biology and Parkinson's disease. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro AA2AR binding assay for ANR-94 typically uses membranes from cells expressing recombinant human AA2AR. Radioligand binding assays are performed using [³H]-CGS-21680 or other AA2AR radioligands. Membranes are incubated with varying concentrations of the test compound (typically 0.1 nM to 10 µM) and a fixed concentration of radioligand in assay buffer for 1-2 hours at room temperature. Non-specific binding is determined in the presence of excess unlabeled AA2AR agonist. Bound radioligand is separated by rapid filtration through glass fiber filters, and radioactivity is measured by liquid scintillation counting. Ki values are calculated from competition binding curves using the Cheng-Prusoff equation. Positive controls and negative controls are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cells expressing AA2AR are treated with ANR-94 at concentrations ranging from 0.1 nM to 10 µM for 1-24 hours, followed by stimulation with an AA2AR agonist. cAMP levels are measured using a competitive ELISA or HTRF-based cAMP detection kit. For antiviral assays, cells (Caco-2, VERO-6) are infected with SARS-CoV-2 in the presence of varying concentrations of the compound, and viral replication is measured by qRT-PCR or plaque assay. Cell viability is assessed using MTT or CellTiter-Glo assays. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, rodent models of Parkinson's disease (e.g., 6-OHDA-lesioned rats, MPTP-treated mice) are used. ANR-94 is administered orally or intraperitoneally at doses ranging from 1 to 30 mg/kg. Motor function is assessed using behavioral tests such as the rotarod test, open field test, and apomorphine-induced rotation test. Neuroprotection is assessed by measuring dopamine levels in the striatum and by immunohistochemical analysis of tyrosine hydroxylase-positive neurons. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of ANR-94 have been partially characterized. The compound has a molecular weight of 207.23 and a molecular formula of C9H13N5O. Following oral or intraperitoneal administration, the compound shows moderate absorption with a Tmax of 1-3 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including brain, consistent with its central nervous system activity. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of ANR-94 are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 30 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| Additional Infomation |
ANR-94 is a potent and specific adenosine A2A receptor antagonist with a Ki of 46 nM for hAA2AR. It may be used for studying Parkinson's disease and also exhibits antiviral activity against SARS-CoV-2. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use. Its potent AA2AR antagonism makes it a valuable tool for studying AA2AR biology, Parkinson's disease, and viral infection.
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| Molecular Formula |
C9H13N5O
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|---|---|
| Molecular Weight |
207.23242
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| Exact Mass |
207.112
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| Elemental Analysis |
C, 52.16; H, 6.32; N, 33.79; O, 7.72
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| CAS # |
634924-89-3
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| PubChem CID |
11805896
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| Appearance |
Solid powder
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| LogP |
1.408
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
15
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| Complexity |
215
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1=C2N=C(OCC)N(CC)C2=NC=N1
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| InChi Key |
QUGDTMONBLMLLD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H13N5O/c1-3-14-8-6(7(10)11-5-12-8)13-9(14)15-4-2/h5H,3-4H2,1-2H3,(H2,10,11,12)
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| Chemical Name |
8-ethoxy-9-ethylpurin-6-amine
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| Synonyms |
ANR-94, ANR94, ANR 94
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~50 mg/mL (~241.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.06 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 (12.06 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 (12.06 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 | 4.8256 mL | 24.1278 mL | 48.2556 mL | |
| 5 mM | 0.9651 mL | 4.8256 mL | 9.6511 mL | |
| 10 mM | 0.4826 mL | 2.4128 mL | 4.8256 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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