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MRS 1523

产品编号 T16135 CAS 212329-37-8

MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 nM for human and rat A3 receptors, respectively). In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively.

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MRS 1523, CAS 212329-37-8

规格	价格/CNY		货期	数量
1 mg	￥ 980		35日内发货
5 mg	￥ 3,290		35日内发货

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化学信息

存储 & 溶解度

参考文献

产品描述	MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 nM for human and rat A3 receptors, respectively). In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively.
靶点活性	A3 receptor (rat):113 nM(ki), A1 receptor:15.6 μM(ki), A2A receptor:2.05 μM, A3 receptor (human):(ki)18.9 nM
体外活性	NECA-induced migration is blocked in dose-response fashion by MRS 1523 with calculated Ki of 147 nM[4]. When human endothelial progenitor cells (hEPC) are co-incubated with MRS 1523 (1 nM), a partial blockade of the adenosine-5'-N-ethylcarboxamide (NECA)-induced migration is observed. Furthermore, in 3-days hEPC, the treatment with MRS 1523 100 nM inhibits the NECA-induced migration by 70%. MRS 1523 (0.1-1 μM) treatment obviously 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].
体内活性	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. The endogenous agonist adenosine reduces N-type Ca currents, and its effect is inhibited by 56% in the presence of A3AR antagonist MRS 1523 [2].

分子量	399.55
分子式	C23H29NO3S
CAS No.	212329-37-8

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

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 Arch Pharmacol. 2008 Jun;377(4-6):591-5.

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