TGN-020|51987-99-6|-陌孚医药/Medlife

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TGN-020

目录号: PL06258 纯度: ≥99%

CAS No. :51987-99-6

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中文名称	TGN-020
中文别名	N-(1,3,4-噻二唑)烟酰胺;N-(1,3,4-噻二唑-2-基)吡啶-3-甲酰胺
英文名称	TGN-020
英文别名	N-(1,3,4-Thiadiazolyl)nicotinamide;N-(1,3,4-Thiadiazol-2-yl)nicotinamide;TGN 020;2-(Nicotinamide)-1,3,4-thiadiazole (N-(1,3,4-Thiadiazol-2-yl)-3-pyridinecarboxamide;N-(1,3,4-thiadiazol-2-yl)pyridine-3-carboxamide;2-(Nicotinamide)-1,3,4-thiadiazole;N-(1,3,4-Thiadiazol-2-yl)-3-pyridinecarboxamide;N-(1,3,4-Thiadiazolyl)-m-nicotinamide;TGN-020;N-(1,3,4-Thiadiazol-2-yl)pyridine-3-carboxamide
Cas No.	51987-99-6
分子式	C₈H₆N₄Os
分子量	206.22
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TGN-020 是一种选择性水通道蛋白 4 (AQP4) 抑制剂，IC₅₀ 为 3.1 μM。TGN-020 是一种 PROTAC linker，属于 alkyl chain 类，可用于合成 PROTAC 分子。TGN-020 减轻大鼠脊髓压迫损伤后的水肿并抑制神经胶质瘢痕的形成。
生物活性	TGN-020 is a selective Aquaporin 4 (AQP4) inhibitor with an IC 50 of 3.1 μM. TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.TGN-020 alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats.
性状	Solid
IC50 & Target[1][2]	Alkyl-Chain
体外研究(In Vitro)	PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	TGN-020 (0.02 mg/μL; two microliter intravitreal injections) can suppress retinal edema in STZ-induced diabetic rats (nine-week-old male Wistar rats) retinas. TGN-020 (100?mg/kg; ip; single dose immediately followed SCI) promotes functional recovery at days 3, 7, 14, 21, and 28, as well as reduces the degree of edema and inhibits the expression of AQP4, GFAP, PCNA at days 3 after SCI. TGN-020 inhibits the glial scar formation and upregulates GAP-43 expression in adult female Sprague-Dawley rats (180-220?g, 9-10?weeks old) with SCI. 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]. Vincent J Huber, et al. Identification of aquaporin 4 inhibitors using in vitro and in silico methods. Bioorg Med Chem. 2009 Jan 1;17(1):411-7. [2]. Shou Oosuka, et al. Effects of an Aquaporin 4 Inhibitor, TGN-020, on Murine Diabetic Retina. Int J Mol Sci. 2020 Mar 27;21(7):2324. [3]. An S, et al. Small-molecul

溶解度数据	In Vitro: DMSO : 16.67 mg/mL (80.84 mM; Need ultrasonic)配制储备液

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