VGX-1027

VGX-1027
Identifiers
	IUPAC name 2-(3-phenyl-4,5-dihydro-1,2-oxazol-5-yl)acetic acid;
CAS Number	6501-72-0 ;
PubChem CID	10798271;
ChemSpider	8973577;
UNII	AKT814N13R;
ChEMBL	ChEMBL1320667;
CompTox Dashboard (EPA)	DTXSID50445023 ;
Chemical and physical data
Formula	C11H11NO3
Molar mass	205.213 g·mol−1
3D model (JSmol)	Interactive image;
	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 (GIT-27) is a drug which acts as an immunomodulator. It acts by blocking downstream signalling of the Toll-like receptors TLR2, TLR4 and TLR6, and thereby reducing production of various cytokines, including interleukins and TNF-α. In animal studies it has antiinflammatory effects and has been investigated for conditions such as arthritis and lung inflammation.[1][2][3][4][5][6]

References

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

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

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

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

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

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

[6] Ahmad SF, Nadeem A, Ansari MA, Bakheet SA, Alasmari F, Alasmari AF, et al. (November 2019). "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. 237: 116930. doi:10.1016/j.lfs.2019.116930. PMID 31610190.