[CAS NO. 212329-37-8] MRS1523
PRODUCTS SPECIFICATIONS [212329-37-8]
DESCRIPTION [212329-37-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 399.55 |
| Molecular Formula | C23H29NO3S |
| SMILES | O=C(OCCC)C1=C(C(C(SCC)=O)=C(N=C1C2=CC=CC=C2)CC)CCC |
1 Publications Citing Use of MCE
Summary
MRS 1523 is a potent and selective adenosine A 3 receptor antagonist with K i values of 18.9 nM and 113 nM for human and rat A 3 receptors , respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A 1 and A 2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons [1] [2] .
IC50 & Target
Ki: 18.9 nM (Human A 3 receptor), 113 nM (Rat A 3 receptor), 15.6 µM (A1 receptor) and 2.05 µM (A2A receptor) [1]
In Vitro
MRS 1523 (0.1-1 μM) treatment significantly antagonizes cell numbers to 40.7% and 57.4% of the control values, respectively, 30 min before the addition of cordycepin (60 μM). MRS1523 (1 μM) alone has any effect on tumor cell growth
[3]
.
A partial blockade of the adenosine-5'-N-ethylcarboxamide (NECA)-induced migration is observed when human endothelial progenitor cells (hEPC) are co-incubated with MRS 1523 (1 nM). Furthermore, in 3-days hEPC, the treatment with MRS 1523 100 nM inhibits the NECA-induced migration by 70%. NECA-induced migration is blocked in dose-response fashion by MRS 1523 with calculated K
i
of 147 nM
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [3]
| Cell Line: | B16-BL6 cells |
| Concentration: | 0.1 µM, 1 µM |
| Incubation Time: | 24 hours, 48 hours, 72 hours |
| Result: | Antagonized the growth suppression induced by cordycepin. |
In Vivo
The expression and functional effects of A3 adenosine receptor (A3AR) on the excitability of small- to medium-sized, capsaicin-sensitive, dorsal root ganglion (DRG) neurons isolated from 3- to 4-week-old rats are investigated. The endogenous agonist adenosine reduces N-type Ca currents, and its effect is inhibited by 56% in the presence of A3AR antagonist MRS 1523. Current-clamp recordings demonstrated that neuronal firing of rat DRG neurons was also significantly reduced by A3AR activation in a MRS 1523-sensitive but PD173212-insensitive manner [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Oil
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Pure form | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 250.28 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5028 mL | 12.5141 mL | 25.0282 mL |
| 5 mM | 0.5006 mL | 2.5028 mL | 5.0056 mL |
| 10 mM | 0.2503 mL | 1.2514 mL | 2.5028 mL |
References
- [1] Li AH, et al. Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.J Med Chem. 1998 Aug 13;41(17):3186-201.
- [2] Coppi E, et al. Adenosine A3 receptor activation inhibits pronociceptive N-type Ca2+ currents and cell excitability in dorsal root ganglion neurons.Pain. 2019 May;160(5):1103-1118.
- [3] Fernandez P, et al. Adenosine A₂A and A₃ receptors are involved in the human endothelial progenitor cells migration. J Cardiovasc Pharmacol. 2012 May;59(5):397-404.
- [4] Yoshikawa N, et al. Cordycepin (3'-deoxyadenosine) inhibits the growth of B16-BL6 mouse melanoma cells through the stimulation of adenosine A3 receptor followed by glycogen synthase kinase-3beta activation and cyclin D1 suppression. Naunyn Schmiedebergs A
Synonyms