MRS 1523
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- CAS号:
- 212329-37-8
- 英文名:
- MRS 1523
- 英文别名:
- MRS 1523 >98% (HPLC);UUSHFEVEROROSP-UHFFFAOYSA-N;3-propyl-6-ethyl-5-[(ethylthio)carbonyl]-2 phenyl-4-propyl-3-pyridine carboxylate;3-Pyridinecarboxylic acid, 6-ethyl-5-[(ethylthio)carbonyl]-2-phenyl-4-propyl-, propyl ester
- 中文名:
- MRS 1523
- 中文别名:
- 化合物 T16135;可分装 5000/100MG
- CBNumber:
- CB8497073
- 分子式:
- C23H29NO3S
- 分子量:
- 399.55
- MOL File:
- 212329-37-8.mol
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MRS 1523化学性质
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沸点:
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551.3±50.0 °C(Predicted)
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密度:
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1.100±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: >10 mg/mL
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酸度系数(pKa):
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1.44±0.28(Predicted)
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形态:
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oil
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颜色:
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colorless to light brown
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MRS 1523性质、用途与生产工艺
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
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Cell Line:
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B16-BL6 cells
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Concentration:
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0.1 µM, 1 µM
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Incubation Time:
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24 hours, 48 hours, 72 hours
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Result:
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Antagonized the growth suppression induced by cordycepin.
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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.
MRS 1523
上下游产品信息
上游原料
下游产品
212329-37-8, MRS 1523 相关搜索:
- 可分装 5000/100MG
- 化合物 T16135
- 212329-37-8
- MRS 1523 >98% (HPLC)
- 3-Pyridinecarboxylic acid, 6-ethyl-5-[(ethylthio)carbonyl]-2-phenyl-4-propyl-, propyl ester
- UUSHFEVEROROSP-UHFFFAOYSA-N
- 3-propyl-6-ethyl-5-[(ethylthio)carbonyl]-2 phenyl-4-propyl-3-pyridine carboxylate