| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87244-10mg促销 |
≥98%(HPLC) | ￥319.00 ￥286.00 |
10 | - | - | - | - |
|
S87244-25mg促销 |
≥98%(HPLC) | ￥582.00 ￥524.00 |
10 | - | - | - | - |
|
S87244-50mg促销 |
≥98%(HPLC) | ￥755.00 ￥679.00 |
7 | - | - | - | - |
|
S87244-100mg促销 |
≥98%(HPLC) | ￥956.00 ￥860.00 |
5 | - | - | - | - |
|
| 产品描述： | TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent brain peneration and moderate bioavailability in rats | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | OX1 Receptor：3 nM (Ki)；OX2 Receptor：0.2 nM (Ki);OXReceptor | ||||||||||||||||||||
| 体内研究： | TCS 1102 (compound 18) (15, 50, 100 mg/kg; i.p; single dose) induces locomotion inhibition in rat in a dose dependent manner. TCS-1102 (10 and 20 mg/kg; i.p.; single dose) decreases fear and anxiety in rats after exposure to footshock. Furthermore, TCS-1102 (10 mg/kg; i.p.; single dose) also shows anxiolytic effects for high responders (HR) rat when tested in the elevated T-maze. PK of TCS 1102 in Rat (100 mg/kg; i.p.; measured at 30 min) Animal Model: Male Sprague–Dawley rats (130-160 g) Dosage: 10 and 20 mg/kg Administration: Intraperitoneal injection; 30 min before received the footshocks Result: Decreased fear and anxiety in rats 14 days after exposure to footshock. | ||||||||||||||||||||
| 参考文献： | 1. Bergman JM, et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. 2. Turku A, et al. Orexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity. PLoS One. 2017 Jun 2;12(6):e0178526. 3. Chen X, et al. Orexins (hypocretins) contribute to fear and avoidance in rats exposed to a single episode of footshocks. Brain Struct Funct. 2013 Aug 18. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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