MRS 1523|cas:212329-37-8|西域试剂

MRS 1523,99.93%

产品编号：Bellancom-121119| CAS NO：212329-37-8| 分子式：C₂₃H₂₉NO₃S| 分子量：399.55

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货号	价格	库存与货期
Bellancom-121119	￥1900.00	杭州北京（现货）
Bellancom-121119	￥3200.00	杭州北京（现货）
Bellancom-121119	￥7000.00	杭州北京（现货）
Bellancom-121119	￥12000.00	杭州北京（现货）

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MRS 1523

产品介绍

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 K_i 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 A_2A 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。

生物活性

MRS 1523 is a potent and selective adenosine A₃ receptor antagonist with K_i values of 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 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.

体外研究

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Oil

溶解性数据

In Vitro:

DMSO : 100 mg/mL (250.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。