| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
LUF5834 targets adenosine receptors, specifically acting as an A2A and A2B adenosine receptor partial agonist. It has an EC50 of 12 nM and shows 45-fold selectivity over the adenosine A3 receptor. The compound is also a partial agonist at A1/A2A receptors. Adenosine receptors are G protein-coupled receptors involved in numerous physiological processes.
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| ln Vitro |
LUF5834 is a potent A2A and A2B adenosine receptor agonist with an EC50 of 12 nM. It has 45-fold selectivity over the adenosine A3 receptor. The compound is also a partial agonist at A1/A2A receptors. Its activity at adenosine receptors modulates cAMP levels and downstream signaling pathways.
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| ln Vivo |
Specific in vivo efficacy data for LUF5834 are not extensively detailed in standard reference sources. As an adenosine receptor agonist, it would be expected to produce effects related to adenosine receptor activation, such as vasodilation, anti-inflammatory effects, and modulation of neurotransmitter release. Studies in animal models would be required to evaluate its in vivo pharmacological profile.
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| Enzyme Assay |
LUF5834's binding affinity to adenosine receptors can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant human adenosine receptors. Competition binding experiments are performed with increasing concentrations of LUF5834 against a fixed concentration of a radiolabeled adenosine receptor ligand (e.g., [³H]ZM241385 for A2A or [³H]DPCPX for A1). Ki values are calculated from competition curves.
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| Cell Assay |
The functional activity of LUF5834 at adenosine receptors is evaluated in vitro using cell lines expressing recombinant adenosine receptors (e.g., CHO or HEK293 cells expressing A2A or A2B receptors). Cells are treated with increasing concentrations of LUF5834, and the stimulation of cAMP accumulation is measured using a cAMP ELISA or homogeneous time-resolved fluorescence (HTRF) assay. The EC50 for cAMP production is determined. Partial agonism is confirmed by comparing the maximal response to that of a full agonist (e.g., NECA).
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| Animal Protocol |
LUF5834 would be administered to animal models via appropriate routes (e.g., intraperitoneal, intravenous, or oral) to evaluate its in vivo effects. Depending on the indication, models of inflammation, cardiovascular disease, or neurological disorders could be used. Physiological parameters (e.g., blood pressure, heart rate, inflammatory markers) would be measured to assess adenosine receptor-mediated effects.
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| ADME/Pharmacokinetics |
LUF5834 has a molecular weight of 348.38 and molecular formula C17H12N6OS. It should be stored at 2-8°C. Its SMILES string is C(#N)C=1C(=C(C#N)C(N)=NC1SCC=2NC=CN2)C3=CC=C(O)C=C3. Specific pharmacokinetic parameters are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of LUF5834 is not extensively documented. As an adenosine receptor agonist, potential adverse effects may include cardiovascular effects (e.g., hypotension, bradycardia) and CNS effects (e.g., sedation). Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
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| Additional Infomation |
LUF5834 (CAS# 333962-91-7) is a potent A2A and A2B adenosine receptor partial agonist with an EC50 of 12 nM. It shows 45-fold selectivity over the adenosine A3 receptor. The compound is also known as LUF-5834. It is a research tool for studying adenosine receptor signaling and pharmacology.
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| Molecular Formula |
C17H12N6OS
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|---|---|
| Molecular Weight |
348.38
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| Exact Mass |
348.079
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| CAS # |
333962-91-7
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| PubChem CID |
135543624
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| Appearance |
White to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
655.8±65.0 °C at 760 mmHg
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| Flash Point |
350.4±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.753
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| LogP |
2.75
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
548
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| Defined Atom Stereocenter Count |
0
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| Synonyms |
LUF 5834; LUF-5834; LUF5834
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8704 mL | 14.3521 mL | 28.7043 mL | |
| 5 mM | 0.5741 mL | 2.8704 mL | 5.7409 mL | |
| 10 mM | 0.2870 mL | 1.4352 mL | 2.8704 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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