| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
The primary target of MRS1220 is the human adenosine A3 receptor (hA3AR). It is a potent and highly selective antagonist at this receptor. It specifically binds to the A3AR, preventing adenosine from activating it. This selective inhibition allows researchers to study the specific roles of the A3AR in various biological processes.
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| ln Vitro |
In the human macrophage U-937 cell line, MRS 1220 reverses the inhibitory impact of A3 agonists on tumor necrosis factor-α production with an IC50 of 0.3 μM [1]. U87MG glioma stem cells (GSC) showed a 25% reduction in VEGF release following a 72-hour hypoxic period when treated with MRS1220 [2].
In vitro, MRS1220 exhibits high affinity for the human A3 adenosine receptor with a Ki of 0.59 nM. It shows significantly lower affinity for rat A1 (305 nM) and rat A2A (52 nM) receptors. It exhibits an IC₅₀ value >1 µM for inhibition of binding to rat A3 receptors. |
| ln Vivo |
In vivo, MRS1220 (0.15 mg/kg; i.p.) decreases tumor growth and vascularization. In vivo, MRS1220 demonstrates strong anti-angiogenic properties [2].
In vivo, MRS1220 reduces tumor size and angiogenesis in glioblastoma models. As a selective A3AR antagonist, it modulates adenosine signaling in the central nervous system and has therapeutic potential for CNS diseases. Detailed in vivo data are available from research publications. |
| Enzyme Assay |
For in vitro receptor binding assays, MRS1220 is evaluated for its ability to compete with radiolabeled adenosine receptor ligands. Standard protocols involve incubating membrane preparations from cells expressing A3AR with varying concentrations of MRS1220 (0.01-1000 nM) and radiolabeled antagonist. Ki values are calculated from competition curves.
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| Cell Assay |
Cell viability assay [2]
Cell Types: U87MG GSC Tested Concentrations: 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: VEGF secretion diminished by approximately 25%. Cell-based assays for MRS1220 involve treating cells expressing A3AR with the compound at concentrations of 0.01-1000 nM. Receptor-mediated signaling (e.g., cAMP accumulation) is measured to assess antagonist activity. Selectivity is confirmed by testing against other adenosine receptor subtypes. |
| Animal Protocol |
Animal/Disease Models: 8 male SD (SD (Sprague-Dawley)) rats harboring C6 (GSC)[2]
Doses: 0.15 mg/kg/72 h Route of Administration: intraperitonealinoculation for 15 days Experimental Results: Reduction close to 80% and consistent with vehicle Compared with the medical treatment group, the tumor volume was diminished by 90% on the 10th and 15th days after treatment respectively. In vivo studies with MRS1220 are conducted in rodent models of glioblastoma or CNS diseases. Typical protocols involve administering the compound intraperitoneally or orally at doses of 1-10 mg/kg. Efficacy is assessed by tumor size measurement, angiogenesis assessment, or behavioral endpoints. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of MRS1220 have been characterized in preclinical studies. The compound is likely to have reasonable bioavailability. It distributes to the central nervous system. Detailed PK parameters are available from research publications.
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| Toxicity/Toxicokinetics |
Toxicology data for MRS1220 are available from preclinical studies. The compound is generally well-tolerated at therapeutic doses. Comprehensive toxicology data are available from research publications.
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| References | |
| Additional Infomation |
N-[9-chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide is a member of the quinazolin class of compounds.
MRS1220 is a potent and selective human A3 adenosine receptor antagonist. Synonyms include N-(9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)-2-phenylacetamide. It has therapeutic potential for CNS diseases. No FDA approvals exist. |
| Molecular Formula |
C21H14CLN5O2
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|---|---|
| Molecular Weight |
403.83
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| Exact Mass |
403.084
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| CAS # |
183721-15-5
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| Related CAS # |
183721-15-5;
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| PubChem CID |
393595
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| Appearance |
White to off-white solid powder
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| Density |
1.49g/cm3
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| Index of Refraction |
1.744
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| LogP |
4.445
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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 |
4
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| Heavy Atom Count |
29
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| Complexity |
589
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC2=C(C3=NC(C4=CC=CO4)=NN3C(NC(=O)CC3C=CC=CC=3)=N2)C=1
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| InChi Key |
TWWFAXQOKNBUCR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H14ClN5O2/c22-14-8-9-16-15(12-14)20-25-19(17-7-4-10-29-17)26-27(20)21(23-16)24-18(28)11-13-5-2-1-3-6-13/h1-10,12H,11H2,(H,23,24,28)
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| Chemical Name |
N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide
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| Synonyms |
MRS 1220 MRS-1220 MRS1220
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~4 mg/mL (~9.91 mM)
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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 | 2.4763 mL | 12.3814 mL | 24.7629 mL | |
| 5 mM | 0.4953 mL | 2.4763 mL | 4.9526 mL | |
| 10 mM | 0.2476 mL | 1.2381 mL | 2.4763 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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