Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約6-8 週間 | ¥ 349,000 |
50 mg | 約6-8 週間 | ¥ 454,500 |
100 mg | 約6-8 週間 | ¥ 574,000 |
説明 | Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1]. |
In vitro | Compound 12d, an adenosine receptor inhibitor, demonstrates metabolic stability with 96.56% and 97.97% of the parent compound remaining after a 120-minute incubation with mouse liver microsomes (MLMs) and rat liver microsomes (RLMs), respectively [1]. |
In vivo | Adenosine receptor inhibitor 1 administered intraperitoneally (i.p.) at doses of 20, 30, 40 mg/kg demonstrated concentration-dependent antinociceptive effects, reducing the pain response in animal models. Specifically, at a 20 mg/kg dose, it exhibited an anti-inflammatory effect, reducing edema in a carrageenan-induced model, and at doses of 5, 10, 20 mg/kg, it showed significant analgesic effects in mice, reducing pain from peripheral sources. In an 18-26 g male albino Swiss mouse model with chronic pain induced by 5% formalin, doses of 20, 30, 40 mg/kg decreased the licking/biting time of the irritated paw. In 150-180 g male Wistar rats experiencing carrageenan-induced edema, a 20 mg/kg dose inhibited edema by 23.3%, 54.2%, and 66.0% over 1, 2, and 3 hours, respectively. Furthermore, in mice injected with irritants such as phenylbenzoquinone or acetic acid to induce pain, doses of 5, 10, 20 mg/kg led to a decrease in pain manifestations by 32.9%, 54.9%, and 82.0%, respectively. |
分子量 | 395.82 |
分子式 | C17H19ClFN5O3 |
CAS No. | 2550400-52-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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Adenosine receptor inhibitor 1 2550400-52-5 Inhibitor inhibitor inhibit