| Bioactivity | VGX-1027 is an orally active isoxazole compound that exhibits various immunomodulatory properties. VGX-1027 targets macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, IL-10. VGX-1027 has antidiabetogenic effects by limiting cytokine-mediated immunoinflammatory events[1][2][3]. | ||||||||||||
| Invitro | VGX-1027 (37.5, 75, 150, 300 μM; for 24 h) does not affect the viability of tumor cells，including the three malignant rodent cell lines (mouse fibrosarcoma L929, rat astrocytoma C6, and mouse melanoma B16) and the four human cell lines (adenocarcinoma HeLa, breast carcinoma BT20, colon carcinoma LS174, and glioblastoma U251)[2]. | ||||||||||||
| In Vivo | VGX-1027 (10, 20 mg/kg of i.p. for 12 day or 100 mg/kg of p.o. for 11 day) successfully counteractes the development of destructive insulitis and hyperglycemia[1]. VGX-1027 (25 mg/kg; ip; single dose) counteracts the uveitis-inducing effect of LPS in eight-week-old male Lewis rats (180-220 g)[3]. Animal Model: | ||||||||||||
| Name | VGX-1027 | ||||||||||||
| CAS | 6501-72-0 | ||||||||||||
| Formula | C11H11NO3 | ||||||||||||
| Molar Mass | 205.21 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Stosic-Grujicic S, 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. [2]. Danijela Maksimovic-Ivanic, et al. Anticancer properties of the novel nitric oxide-donating compound (S,R)-3-phenyl-4,5-dihydro-5-isoxazole acetic acid-nitric oxide in vitro and in vivo. Mol Cancer Ther. 2008 Mar;7(3):510-20. [3]. K Mangano, et al. Effects of the immunomodulator, VGX-1027, in endotoxin-induced uveitis in Lewis rats. Br J Pharmacol. 2008 Nov;155(5):722-30. |