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VGX-1027

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Chemical Structure| 6501-72-0 同义名 : GIT 27
CAS号 : 6501-72-0
货号 : A590582
分子式 : C11H11NO3
纯度 : 99%+
分子量 : 205.21
MDL号 : MFCD08696167
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 55 mg/mL(268.02 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+5% Tween 80+water 10 mg/mL

生物活性
描述 VGX-1027 is a small molecule, isoxazoline compound that can decrease the production of tumor necrosis factor-α production from macrophages in response to the activation of Toll-like receptors. It has been shown to significantly downregulate the expression of MHC class II molecules, including HLA-DPB1, HLA-DOB, HLA-DRA, IFNG, HIST2H2AB, HIST1H2BM, and FCGR3A at a concentration of 10μM. VGX-1027 treatment also significantly suppressed lipopolysaccharide-induced upregulation of cytokine (e.g. interleukin-22) and chemokines (e.g. CCL8). In the NZB/NZW F1 mouse model of systemic lupus erythematosus, daily intraperitoneal administration with 5mg VGX-1027 for 20 weeks reduced proteinuria and prolonged survival of mice compared with the vehicle-treated control group. Treatment of NZB/NZW F1 mice with VGX-1027 (20mg/day, intraperitoneal injection) for 20 weeks reduced anti-dsDNA autoantibodies in the serum, downregulated cytokine production, and suppressed the development of nephritis compared with the controls[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.87mL

0.97mL

0.49mL

24.37mL

4.87mL

2.44mL

48.73mL

9.75mL

4.87mL
参考文献

[1]Stosic-Grujicic S, Cvetkovic I, et al. A potent immunomodulatory compound, (S,R)-3-Phenyl-4,5-dihydro-5-isoxazole acetic acid, prevents spontaneous and accelerated forms of autoimmune diabetes in NOD mice and inhibits the immunoinflammatory diabetes induced by multiple low doses of streptozotocin in CBA/H mice. J Pharmacol Exp Ther. 2007 Mar;320(3):1038-49. Epub 2006 Dec 5. Erratum in: J Pharmacol Exp Ther. 2007 Apr;321(1):420

[2]Stojanovic I, Cuzzocrea S, et al. In vitro, ex vivo and in vivo immunopharmacological activities of the isoxazoline compound VGX-1027: modulation of cytokine synthesis and prevention of both organ-specific and systemic autoimmune diseases in murine models. Clin Immunol. 2007 Jun;123(3):311-23.

[3]Fagone P, Muthumani K, Mangano K, Magro G, Meroni PL, Kim JJ, Sardesai NY, Weiner DB, Nicoletti F. VGX-1027 modulates genes involved in lipopolysaccharide-induced Toll-like receptor 4 activation and in a murine model of systemic lupus erythematosus. Immunology. 2014 Aug;142(4):594-602.