2. GPCR/G Protein
  3. Adenosine Receptor
  4. MRS1220

MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.

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MRS1220 Chemical Structure

MRS1220 Chemical Structure

CAS No. : 183721-15-5

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Based on 1 publication(s) in Google Scholar

MRS1220 Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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Description

MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2].

In Vitro

MRS 1220 reverses the effect of A3 agonist-elicited inhibition of tumor necrosis factor-α formation in the human macrophage U-937 cell line with an IC50 of 0.3 μM[1].
VEGF secretion in U87MG glioblastoma stem-like cells (GSCs) decreases ~25% with MRS1220 after 72 h of hypoxia[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MRS1220 Related Antibodies

Cell Viability Assay[2]

Cell Line: U87MG GSCs
Concentration: 10 μM
Incubation Time: 72 hours
Result: Decreased ~25% VEGF secretion.
In Vivo

MRS1220 (0.15 mg/kg; intraperitoneal inoculation) reduces tumor size and blood vessel formation in vivo. MRS1220 exhibits a strong in vivo anti-angiogenic effect[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight, 8 week-old male Sprague-Dawley rats bearing C6 (GSCs)[2]
Dosage: 0.15 mg/kg/72 h
Administration: Administered by intraperitoneal inoculation, for fifteen days
Result: A reduction close to 80% and 90% in tumor volume compared to the vehicle-treated group at day ten and fifteen post-treatment, respectively.
Molecular Weight

403.82

Formula

C21H14ClN5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC2=C(C=C(Cl)C=C2)C3=NC(C4=CC=CO4)=NN13)CC5=CC=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 4 mg/mL (9.91 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4764 mL 12.3818 mL 24.7635 mL
5 mM 0.4953 mL 2.4764 mL 4.9527 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4764 mL 12.3818 mL 24.7635 mL 61.9088 mL
5 mM 0.4953 mL 2.4764 mL 4.9527 mL 12.3818 mL
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MRS1220 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MRS1220183721-15-5MRS 1220MRS-1220Adenosine ReceptorP1 receptorA3adenosinereceptorhA3ARdiseasescentralnervoussystemglioblastomatumorsizebloodvesselformationInhibitorinhibitorinhibit

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