MRS 1523

MRS 1523

中文名称MRS 1523
中文同义词化合物 T16135;可分装 5000/100MG
英文名称MRS 1523
英文同义词3-propyl-6-ethyl-5-[(ethylthio)carbonyl]-2 phenyl-4-propyl-3-pyridine carboxylate;UUSHFEVEROROSP-UHFFFAOYSA-N;3-Pyridinecarboxylic acid, 6-ethyl-5-[(ethylthio)carbonyl]-2-phenyl-4-propyl-, propyl ester;MRS 1523 >98% (HPLC)
CAS号212329-37-8
分子式C23H29NO3S
分子量399.55
EINECS号
相关类别
Mol文件212329-37-8.mol
结构式MRS 1523 结构式

MRS 1523 性质

沸点551.3±50.0 °C(Predicted)
密度1.100±0.06 g/cm3(Predicted)
储存条件2-8°C
溶解度二甲基亚砜:>10 mg/mL
酸度系数(pKa)1.44±0.28(Predicted)
形态油状
颜色无色至浅棕色

MRS 1523 用途与合成方法

MRS 1523 是一种有效的选择性腺苷 A3 受体拮抗剂,对人和大鼠 A3 受体的 Ki 值分别为 18.9 nM 和 113 nM。在大鼠中,MRS 1523 对 A3 的选择性分别是 A1 和 A2A 受体的 140 倍和 18 倍。MRS 1523 可以通过 N-type Ca channel 阻滞和抑制大鼠背根神经节神经元的动作电位而发挥抗痛觉过敏作用。

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)

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.
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.

Cell Viability Assay

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.

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.

安全信息

WGK Germany3

MSDS信息

MRS 1523 上下游产品信息

"MRS 1523"相关产品信息
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