Facinicline hydrochloride|677305-02-1|(RG3487 hydrochloride)-陌孚医药/Medlife

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Facinicline hydrochloride (Synonyms: RG3487 hydrochloride)

目录号: PL07656 纯度: ≥99%

CAS No. :677305-02-1

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中文名称	Facinicline hydrochloride
英文名称	Facinicline hydrochloride
英文别名	Facinicline hydrochloride;O6J463N18M;N-((3S)-1-Azabicyclo(2.2.2)oct-3-yl)-1H-indazole-3-carboxamide hydrochloride;RG3487;N-[(3s)-1-azabicyclo[2.2.2]oct-3-yl]-1h-indazole-3-carboxamide hydrochloride;MEM 3454;Q27285409;1H-Indazole-3-carboxamide, N-(3S)-1-azabicyclo(2.2.2)oct-3-yl-, monohydrochloride;1H-Indazole-3-carboxamide, N-(3S)-1-azabicyclo(2.2.2)oct-3-yl-, hydrochloride (1:1);RG3487 hydrochloride
Cas No.	677305-02-1
分子式	C₁₅H₁₉ClN₄O
分子量	306.79
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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 K_i 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K_i 值为 1.2 nM。
生物活性	Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a K i of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT 3 Rs with a K i value of 1.2 nM.
性状	Solid
IC50 & Target[1][2]	5-HT3 Receptor 1.2 nM (Ki) α7 6 nM (Ki)
体外研究(In Vitro)	Facinicline (RG3487) activates human α7 nAChRs with an EC50 of 0.8 μM (oocytes) and 7.7 μM (QM7 cells). Facinicline (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC50 2.8 nM (oocytes), 32.7 nM (N1E-115 cells)). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Tanya L Wallace, et al. RG3487, a Novel Nicotinic α7 Receptor Partial Agonist, Improves Cognition and Sensorimotor Gating in Rodents. J Pharmacol Exp Ther. 2011 Jan;336(1):242-53.

溶解度数据	In Vitro: DMSO : 125 mg/mL (407.44 mM; Need ultrasonic)H₂O : 100 mg/mL (325.96 mM; Need ultrasonic)配制储备液

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