MRS-1191 |
| رقم الكتالوجGC38112 |
MRS-1191 هو أحد مضادات مستقبلات الأدينوزين A3 القوية والانتقائية بقيمة KB تبلغ 92 نانومتر ، وقيمة Ki تبلغ 31.4 نانومتر لمستقبل A3 البشري و IC50 من 120 نانومتر لخلايا CHO
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Cas No.: 185222-90-6
Sample solution is provided at 25 µL, 10mM.
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MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells[1].
The effects of putative A3 adenosine receptor antagonist of MRS-1191 is characterized in receptor binding and functional assays. MRS-1191 is found to be competitive in saturation binding studies using the agonist radioligand [125I]AB-MECA (N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide) at cloned human brain A3 receptor expressed in HEK-293 cells. Antagonism is demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of [35S]guanosine 5'-O-(3-thiotriphosphate) ([35S]GTP-gamma-S) to the associated G-proteins. MRS-1191 with a KB value of 92 nM, proves to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase[1].
[1]. Jacobson KA, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.
| Cas No. | 185222-90-6 | SDF | |
| Canonical SMILES | O=C(OCC)C1=C(NC(C2=CC=CC=C2)=C(C1C#CC3=CC=CC=C3)C(OCC4=CC=CC=C4)=O)C | ||
| Formula | C31H27NO4 | M.Wt | 477.55 |
| الذوبان | DMSO: 250 mg/mL (523.51 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.094 mL | 10.4701 mL | 20.9402 mL |
| 5 mM | 0.4188 mL | 2.094 mL | 4.188 mL |
| 10 mM | 0.2094 mL | 1.047 mL | 2.094 mL |
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- Purity: >98.50%
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