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Facinicline hydrochloride (RG3487) 是一种口服有效的烟碱α7 receptor 部分激动剂,对人 nAChR 的 Ki 值为 6 nM。它可改善啮齿类动物的认知和感觉运动门控。它与5-HT3受体结合的 Ki 为 1.2 nM。
Facinicline hydrochloride (RG3487) 是一种口服有效的烟碱α7 receptor 部分激动剂,对人 nAChR 的 Ki 值为 6 nM。它可改善啮齿类动物的认知和感觉运动门控。它与5-HT3受体结合的 Ki 为 1.2 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 472 | 现货 | |
5 mg | ¥ 1,190 | 现货 | |
10 mg | ¥ 1,910 | 现货 | |
25 mg | ¥ 3,150 | 现货 | |
50 mg | ¥ 4,360 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,300 | 现货 |
产品描述 | Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM). Facinicline hydrochloride improves cognition and sensorimotor gating in rodents. |
靶点活性 | 5-HT3 receptor:1.2 nM (Ki), α7 nAChR:6 nM (Ki) |
体外活性 | Facinicline hydrochloride exhibits antagonist properties at the serotonin 3 receptor in oocytes(IC50 = 2.8 μM) and N1E-115 cells(IC50 = 32.7 μM)[2].Facinicline hydrochloride activates human α7 nAChRs in oocytes(EC50 = 0.8 μM) and QM7 cells(EC50 = 7.7 μM)[2]. |
体内活性 | In Male Sprague-Dawley rats, Facinicline hydrochloride (0.1–10 mg/kg p.o.) selectively enhances object recognition memory[1]. Facinicline hydrochloride improves object recognition memory in rats after acute(1.0 mg/kg p.o.) or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range[2]. |
别名 | RG3487 |
分子量 | 306.79 |
分子式 | C15H19ClN4O |
CAS No. | 677305-02-1 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 100 mg/mL (325.96 mM) DMSO: 125 mg/mL (407.44 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
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