VGX-1027

VGX-1027
识别信息
	IUPAC命名法 2-(3-phenyl-4,5-dihydro-1,2-oxazol-5-yl)acetic acid; ;
CAS号	6501-72-0
PubChem CID	10798271;
ChemSpider	8973577;
UNII	AKT814N13R;
ChEMBL	ChEMBL1320667;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID50445023 ;
化学信息
化学式	C11H11NO3
摩尔质量	205.21 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES C1C(ON=C1C2=CC=CC=C2)CC(=O)O;
	InChI InChI=1S/C11H11NO3/c13-11(14)7-9-6-10(12-15-9)8-4-2-1-3-5-8/h1-5,9H,6-7H2,(H,13,14); Key:MUFJHYRCIHHATF-UHFFFAOYSA-N;

VGX-1027也称为GIT-27，分子式为C₁₁H₁₁NO₃，是一种免疫調節劑，可阻断TLR2、TLR4、TLR6等Toll样受体的下游信号，因此可减少白介素、TNF-α等多种细胞因子造成的影响。^[1]^[2]^[3]^[4]^[5]^[6]

参考文献

^ Stojanovic I, Cuzzocrea S, Mangano K, Mazzon E, Miljkovic D, Wang M, 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. Clinical Immunology. June 2007, 123 (3): 311–23. PMID 17449326. doi:10.1016/j.clim.2007.03.004.
^ Cha JJ, Hyun YY, Lee MH, Kim JE, Nam DH, Song HK, et al. Renal protective effects of toll-like receptor 4 signaling blockade in type 2 diabetic mice. Endocrinology. June 2013, 154 (6): 2144–55. PMID 23568555. doi:10.1210/en.2012-2080 .
^ Saurus P, Kuusela S, Lehtonen E, Hyvönen ME, Ristola M, Fogarty CL, et al. Podocyte apoptosis is prevented by blocking the Toll-like receptor pathway. Cell Death & Disease. May 2015, 6 (5): e1752. PMC 4669704 . PMID 25950482. doi:10.1038/cddis.2015.125.
^ Lee JC, Menacherry S, Diehl MC, Giffear MD, White CJ, Juba R, et al. Safety, bioavailability, and pharmacokinetics of VGX-1027-A novel oral anti-inflammatory drug in healthy human subjects. Clinical Pharmacology in Drug Development. March 2016, 5 (2): 91–101. PMID 27138022. S2CID 22577185. doi:10.1002/cpdd.193.
^ Xu M, Li F, Wang M, Zhang H, Xu L, Adcock IM, et al. Protective effects of VGX-1027 in PM_2.5-induced airway inflammation and bronchial hyperresponsiveness. European Journal of Pharmacology. January 2019, 842: 373–383. PMID 30419239. S2CID 53292202. doi:10.1016/j.ejphar.2018.11.010. hdl:10044/1/66292 .
^ Ahmad SF, Nadeem A, Ansari MA, Bakheet SA, Alasmari F, Alasmari AF, et al. The potent immunomodulatory compound VGX-1027 regulates inflammatory mediators in CD4⁺ T cells, which are concomitant with the prevention of neuroimmune dysregulation in BTBR T⁺ Itpr3^tf/J mice. Life Sciences. November 2019, 237: 116930. PMID 31610190. doi:10.1016/j.lfs.2019.116930.

外部链接

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[1] Stojanovic I, Cuzzocrea S, Mangano K, Mazzon E, Miljkovic D, Wang M, 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. Clinical Immunology. June 2007, 123 (3): 311–23. PMID 17449326. doi:10.1016/j.clim.2007.03.004.

[2] Cha JJ, Hyun YY, Lee MH, Kim JE, Nam DH, Song HK, et al. Renal protective effects of toll-like receptor 4 signaling blockade in type 2 diabetic mice. Endocrinology. June 2013, 154 (6): 2144–55. PMID 23568555. doi:10.1210/en.2012-2080 .

[3] Saurus P, Kuusela S, Lehtonen E, Hyvönen ME, Ristola M, Fogarty CL, et al. Podocyte apoptosis is prevented by blocking the Toll-like receptor pathway. Cell Death & Disease. May 2015, 6 (5): e1752. PMC 4669704 . PMID 25950482. doi:10.1038/cddis.2015.125.

[4] Lee JC, Menacherry S, Diehl MC, Giffear MD, White CJ, Juba R, et al. Safety, bioavailability, and pharmacokinetics of VGX-1027-A novel oral anti-inflammatory drug in healthy human subjects. Clinical Pharmacology in Drug Development. March 2016, 5 (2): 91–101. PMID 27138022. S2CID 22577185. doi:10.1002/cpdd.193.

[5] Xu M, Li F, Wang M, Zhang H, Xu L, Adcock IM, et al. Protective effects of VGX-1027 in PM_2.5-induced airway inflammation and bronchial hyperresponsiveness. European Journal of Pharmacology. January 2019, 842: 373–383. PMID 30419239. S2CID 53292202. doi:10.1016/j.ejphar.2018.11.010. hdl:10044/1/66292 .

[6] Ahmad SF, Nadeem A, Ansari MA, Bakheet SA, Alasmari F, Alasmari AF, et al. The potent immunomodulatory compound VGX-1027 regulates inflammatory mediators in CD4⁺ T cells, which are concomitant with the prevention of neuroimmune dysregulation in BTBR T⁺ Itpr3^tf/J mice. Life Sciences. November 2019, 237: 116930. PMID 31610190. doi:10.1016/j.lfs.2019.116930.

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