S-Facinicline
| 中文名称 | S-Facinicline |
|---|---|
| 中文同义词 | 化合物 RG3487 HYDROCHLORIDE;化合物FACINICLINE HYDROCHLORIDE |
| 英文名称 | S-Facinicline |
| 英文同义词 | S-Facinicline;Facinicline hydrochloride;RG3487 hydrochloride;RG3487;Inhibitor,nAChR,serotonin 3 receptor,Nicotinic acetylcholine receptors,Serotonin Receptor,5-HT Receptor,inhibit,recognition,5-hydroxytryptamine Receptor,Facinicline,Facinicline hydrochloride,receptor,RG-3487,memory,RG 3487,nicotinic |
| CAS号 | 677305-02-1 |
| 分子式 | C15H19ClN4O |
| 分子量 | 306.79056 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 677305-02-1.mol |
| 结构式 |  |
S-Facinicline 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMSO：125mg/mL（407.44mM）；甲醇：25 mg/mL (81.49 mM) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
Facinicline hydrochloride (RG3487 hydrochloride) 是具有口服活性的烟碱 α7 receptor 部分激动剂，对人nAChR 的 Ki 值为 6 nM。Facinicline hydrochloride (RG3487 hydrochloride) 可改善啮齿类动物的认知和感觉运动门控。Facinicline hydrochloride (RG3487 hydrochloride) 对5-HT3 受体 (拮抗剂)的Ki 值为 1.2 nM。
|
5-HT 3 Receptor 1.2 nM (Ki) |
α7 6 nM (Ki) |
Facinicline (RG3487) activates human α7 nAChRs with an EC
50
of 0.8 μM (oocytes) and 7.7 μM (QM7 cells).
Facinicline (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC
50
2.8 nM (oocytes), 32.7 nM (N1E-115 cells)).
Facinicline (RG3487) improves object recognition memory in rats after acute [minimally effective dose (MED) 1.0 mg/kg p.o.] or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range.
RG3487 (0.1–10 mg/kg p.o.) selectively enhances object recognition memory.
| Animal Model: | Male Sprague-Dawley rats. |
| Dosage: | 0.1-10 mg/kg (Pharmacokinetic Analysis). |
| Administration: | Orally. |
| Result: | The mean C max was typically observed between 0.5 and 4 h. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-108057A | Facinicline hydrochloride | 1 mg | 950元 | |
| 2024/08/19 | HY-108057A | S-Facinicline Facinicline hydrochloride | 677305-02-1 | 5mg | 2400元 |