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Tozadenant (SYN115) 是 A2A 腺苷受体拮抗剂,对人和恒河猴的 Ki 分别为 11.5 和 6 nM。
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Tozadenant (SYN115) 是 A2A 腺苷受体拮抗剂,对人和恒河猴的 Ki 分别为 11.5 和 6 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 153 | 现货 | |
5 mg | ¥ 328 | 现货 | |
10 mg | ¥ 538 | 现货 | |
25 mg | ¥ 987 | 现货 | |
50 mg | ¥ 1,650 | 现货 | |
100 mg | ¥ 2,650 | 现货 | |
200 mg | ¥ 3,880 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 363 | 现货 |
产品描述 | Tozadenant (SYN115) is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively) |
靶点活性 | A2A receptor (rhesus):6 nM(Ki), A2A receptor (human):11.5 nM(Ki) |
体内活性 | 与单独测试的药物相比,Radiprodil和Tozadenant的组合显著提高了MPTP处理的狨猴的运动活性,并改善了其运动障碍。此外,该组合带来的运动功能恢复几乎完全没有不自主运动障碍[1]。 |
动物实验 | Before initiating the Radiprodil & Tozadenant combination experiment, 14 primates were challenged with a dose of 8 mg/kg (po) of L-Dopa and behaviour was recorded for 5 hours. This "Pre-L-Dopa-test" was used to select the 12 subjects required for the study. Their response to the L-Dopa challenge was subsequently used as a comparator to the ensuing response to the different drug treatments and combinations. The effects of the drugs alone or in combination were assessed after acute oral gavage.This experiment investigated the effects on motor deficits of Radiprodil plus Tozadenant twice daily at an interval of 5 hrs according to a modified Latin square design in n = 12 MPTP-treated marmosets. At the time of the second drugs administration a novel object (cotton reel, table tennis ball) was placed into the cage. The four different treatments were (1) Tozadenant (150 mg/kg) plus Radiprodil (2.0 mg/kg), (2) Tozadenant (150 mg/kg) plus vehicle, (3) Radiprodil (2.0 mg/kg) plus vehicle, (4) vehicle[1]. |
别名 | SYN115, 4-羟基-N-[4-甲氧基-7-(4-吗啉基)-2-苯并噻唑基]-4-甲基-1-哌啶甲酰胺 |
分子量 | 406.5 |
分子式 | C19H26N4O4S |
CAS No. | 870070-55-6 |
Smiles | COc1ccc(N2CCOCC2)c2sc(NC(=O)N3CCC(C)(O)CC3)nc12 |
密度 | 1.374 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (123.00 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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