BIA 10-2474|1233855-46-3|-陌孚医药/Medlife

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BIA 10-2474

目录号: PL04935 纯度: ≥99%

CAS No. :1233855-46-3

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中文名称	BIA 10-2474
英文名称	BIA 10-2474
英文别名	5AP1ZW859M;3-(1-(cyclohexyl(methyl)carbamoyl)-1H-imidazol-4-yl)pyridine 1-oxide;1H-Imidazole-1-carboxamide, N-cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-;N-cyclohexyl-N-methyl-4-(1-oxidopyridin-1-ium-3-yl)imidazole-1-carboxamide;example 362 [WO2010074588];GTPL9001;DOWVMJFBDGWVML-UHFFFAOYSA-N;compound 8 l [PubMed: 30113139];AK688478;BIA 10-2474
Cas No.	1233855-46-3
分子式	C₁₆H₂₀N₄O₂
分子量	300.36
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	BIA 10-2474是脂肪酸酰胺水解酶FAAH的抑制剂，对大鼠大脑不同区域的IC₅₀值为50至70mg/kg。
生物活性	BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC 50 values of 50 to 70mg/kg in various rat brain regions.
性状	Solid
IC50 & Target[1][2]	IC50: 50-70mg/kg (FAAH, rat brain regions)
体外研究(In Vitro)	ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70mg/kg (i.p.) in various brain regions. IC50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	In January 2016, severe adverse events (SAE) occurs in the Phase I clinical trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought. 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	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Tong J, et al. Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain. J Cereb Blood Flow Metab. 2016 Sep 20. [2]. Kaur R, et al. What failed BIA 10-2474 Phase I clinical trial? Global speculations and recommendations for future Phase I trials. J Pharmacol Pharmacother. 2016 Jul-Sep;7(3):120-6

溶解度数据	In Vitro: DMSO : 2.2 mg/mL (7.32 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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