Biological Activity
A potent and highly selective antagonist at the human A3 adenosine receptor (Ki values are 0.65, 305, and 52 nM at hA3, rA1 and rA2A respectively. Displays an IC50 value > 1 μM for inhibition of binding to rat A3 receptors).
Licensing Information
Sold with the permission of the NIH, US Patent 60/029,855
Compound Libraries
MRS 1220 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 403.83 |
| Formula | C21H14ClN5O2 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 183721-15-5 |
| PubChem ID | 393595 |
| InChI Key | TWWFAXQOKNBUCR-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C2N=C(NC(=O)CC3=CC=CC=C3)N3N=C(N=C3C2=C1)C1=CC=CO1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.08 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 403.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.48 mL | 12.38 mL | 24.76 mL |
| 5 mM | 0.5 mL | 2.48 mL | 4.95 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.48 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Jacobson et al (1997) Pharmacological characterization of novel A3 adenosine receptor selective antagonists. Neuropharmacology 36 1157 PMID: 9364471
Kim et al (1996) Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) are selective for the human A3 receptor subtype. J.Med.Chem. 39 4142 PMID: 8863790
Kim et al (1998) Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. J.Med.Chem. 41 2835 PMID: 9667972
Keywords: MRS 1220, supplier, potent, selective, hA3, antagonists, Receptors, adenosines, MRS1220, Adenosine, A3, Receptors, Adenosine, A3, Receptors, Tocris Bioscience
