MRS 1191

Modify Date: 2024-03-02 19:21:26

MRS 1191 Structure
MRS 1191 structure
Common Name MRS 1191
CAS Number 185222-90-6 Molecular Weight 477.550
Density 1.2±0.1 g/cm3 Boiling Point 643.1±55.0 °C at 760 mmHg
Molecular Formula C31H27NO4 Melting Point 155 - 156 ℃
MSDS USA Flash Point 342.7±31.5 °C

 Use of MRS 1191


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].

 Names

Name 5-O-benzyl 3-O-ethyl 2-methyl-6-phenyl-4-(2-phenylethynyl)-1,4-dihydropyridine-3,5-dicarboxylate
Synonym More Synonyms

 MRS 1191 Biological Activity

Description 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].
Target

Ki: 31.4 nM (human A3 adenosine receptor)[1]

In Vitro 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].
References

[1]. Jacobson KA, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 643.1±55.0 °C at 760 mmHg
Melting Point 155 - 156 ℃
Molecular Formula C31H27NO4
Molecular Weight 477.550
Flash Point 342.7±31.5 °C
Exact Mass 477.194000
PSA 64.63000
LogP 7.16
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.639
Storage condition -20 °C

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport

 Articles5

More Articles
ATP releases ATP or other nucleotides from human peripheral blood leukocytes through purinergic P2 receptors.

Life Sci. 145 , 85-92, (2016)

Almost every eukaryotic cell releases ATP under certain conditions. The idea that ATP induces the release of ATP has been scantly investigated.We explored this possibility by assessing the rate of exo...

The infarct-sparing effect of IB-MECA against myocardial ischemia/reperfusion injury in mice is mediated by sequential activation of adenosine A3 and A 2A receptors.

Basic Res. Cardiol. 110(2) , 16, (2015)

Conflicting results exist regarding the role of A3 adenosine receptors (A3ARs) in mediating cardioprotection during reperfusion following myocardial infarction. We hypothesized that the effects of the...

Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.

Neuropharmacology 36 , 1157-1165, (1997)

The effects of putative A3 adenosine receptor antagonists of three diverse chemical classes (the flavonoid MRS 1067, the 6-phenyl-1,4-dihydropyridines MRS 1097 and MRS 1191, and the triazoloquinazolin...

 Synonyms

5-Benzyl 3-ethyl 2-methyl-6-phenyl-4-(phenylethynyl)-1,4-dihydropyridine-3,5-dicarboxylate
3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2-methyl-6-phenyl-4-(2-phenylethynyl)-, 3-ethyl 5-(phenylmethyl) ester
mrs1191
5-Benzyl 3-ethyl 2-methyl-6-phenyl-4-(phenylethynyl)-1,4-dihydro-3,5-pyridinedicarboxylate
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