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Submit ReviewMRS 1754 is a selective adenosine A2B receptor antagonist (Ki values are 1.97, 16.8, 403, 503, 570 and 612 nM for hA2B, rA1, hA1, hA2A, hA3 and rA2A receptors respectively).
Sold with the permission of the University of Virginia Patent Foundation
M. Wt | 486.52 |
Formula | C26H26N6O4 |
Storage | Desiccate at RT |
Purity | ≥98% (HPLC) |
CAS Number | 264622-58-4 |
PubChem ID | 6603931 |
InChI Key | AJBBEYXFRYFVNM-UHFFFAOYSA-N |
Smiles | CCCN1C2=C(NC(=N2)C2=CC=C(OCC(=O)NC3=CC=C(C=C3)C#N)C=C2)C(=O)N(CCC)C1=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 2.43 | 5 with gentle warming |
The following data is based on the product molecular weight 486.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.05 mM | 41.11 mL | 205.54 mL | 411.08 mL |
0.25 mM | 8.22 mL | 41.11 mL | 82.22 mL |
0.5 mM | 4.11 mL | 20.55 mL | 41.11 mL |
2.5 mM | 0.82 mL | 4.11 mL | 8.22 mL |
References are publications that support the biological activity of the product.
Kim et al (2000) Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A2B adenosine receptors. J.Med.Chem. 43 1165 PMID: 10737749
Ji et al (2001) [3H]MRS 1754, a selective antagonist radioligand for A2B adenosine receptors. Biochem.Pharmacol. 61 657 PMID: 11266650
Nemeth et al (2007) Adenosine receptor activation ameliorates type I diabetes. FASEB J. 21 2380
If you know of a relevant reference for MRS 1754, please let us know.
Keywords: MRS 1754, MRS 1754 supplier, Selective, A2B, antagonists, Receptors, adenosines, MRS1754, Adenosine, 2752, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for MRS 1754 include:
Wolk et al (2008) Influenza A virus inhibits alveolar fluid clearance in BALB/c mice. PLoS One 178 969 PMID: 18689466
Lemos et al (2015) Adenosine A2B receptor activation stimulates glucose uptake in the mouse forebrain. Purinergic Signal 11 561 PMID: 26446689
Zhan et al (2011) Adenosine A2A and A2B receptors are both required for adenosine A1 receptor-mediated cardioprotection. Am J Physiol Heart Circ Physiol 301 H1183 PMID: 21743001
Hua et al (2011) IL-4 amplifies the pro-inflammatory effect of adenosine in human mast cells by changing expression levels of adenosine receptors. PLoS One 6 e24947 PMID: 21966389
Yu et al (2009) Effect of ventilation pressure on alveolar fluid clearance and β-agonist responses in mice. Am J Respir Crit Care Med 297 L785 PMID: 19684202
He et al (2013) Adenosine regulates bone metabolism via A1, A2A, and A2B receptors in bone marrow cells from normal humans and patients with multiple myeloma. FASEB J 27 3446 PMID: 23682121
Kan et al (2012) Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. J Virol 86 10338 PMID: 22787201
Garção et al (2013) Functional interaction between pre-synaptic α6β2-containing nicotinic and adenosine A2A receptors in the control of DA release in the rat striatum. Br J Pharmacol 169 1600 PMID: 23638679
Gebremedhin et al (2010) Adenosine can mediate its actions through generation of reactive oxygen species. J Cereb Blood Flow Metab 30 1777 PMID: 20531463
Ledderose et al (2016) Adenosine arrests breast cancer cell motility by A3 receptor stimulation. Purinergic Signalling PMID: 27577957
Kohno et al (2015) Anti-inflammatory effects of adenosine N1-oxide. Am J Physiol Lung Cell Mol Physiol 12 2 PMID: 25632271
Welihinda and Amento (2014) Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation. J Inflamm (Lond) 11 37 PMID: 25473378
Pedroza et al (2011) Interleukin-6 contributes to inflammation and remodeling in a model of adenosine mediated lung injury. Mol Vis 6 e22667 PMID: 21799929
Liu et al (2018) Adenosine binds predominantly to adenosine receptor A1 subtype in astrocytes and mediates an immunosuppressive effect. Brain Res 1700 47 PMID: 29935155
Wakisaka et al (2017) An Adenosine Receptor for Olfaction in Fish. Curr Biol 27 1437 PMID: 28502661
Asano (2017) Aminophylline suppresses stress-induced visceral hypersensitivity and defecation in irritable bowel syndrome. Scientific Reports 7 40214 PMID: 28054654
Do you know of a great paper that uses MRS 1754 from Tocris? Please let us know.
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