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VGX-1027

Immunomodulator CAS# 6501-72-0

VGX-1027

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Chemical structure

VGX-1027

3D structure

Chemical Properties of VGX-1027

Cas No. 6501-72-0 SDF Download SDF
PubChem ID 10798271 Appearance Powder
Formula C11H11NO3 M.Wt 205.21
Type of Compound N/A Storage Desiccate at -20°C
Synonyms GIT 27
Solubility DMSO : ≥ 56 mg/mL (272.89 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-(3-phenyl-4,5-dihydro-1,2-oxazol-5-yl)acetic acid
SMILES C1C(ON=C1C2=CC=CC=C2)CC(=O)O
Standard InChIKey MUFJHYRCIHHATF-UHFFFAOYSA-N
Standard 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of VGX-1027

DescriptionOrally active immunomodulatory agent that primarily targets macrophages. Inhibits TNF-α secretion via interference of macrophage toll-like receptor (TLR) 4 and TLR 2/6 signaling pathway. Also reduces the secretion of pro-inflammatory cytokines IL1-β, IL-10 and IFN-γ. Antidiabetogenic; prevents IL-β and IFN-γ-induced pancreatic islet cell death in vitro.

VGX-1027 Dilution Calculator

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VGX-1027 Molarity Calculator

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Preparing Stock Solutions of VGX-1027

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.8731 mL 24.3653 mL 48.7306 mL 97.4611 mL 121.8264 mL
5 mM 0.9746 mL 4.8731 mL 9.7461 mL 19.4922 mL 24.3653 mL
10 mM 0.4873 mL 2.4365 mL 4.8731 mL 9.7461 mL 12.1826 mL
50 mM 0.0975 mL 0.4873 mL 0.9746 mL 1.9492 mL 2.4365 mL
100 mM 0.0487 mL 0.2437 mL 0.4873 mL 0.9746 mL 1.2183 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on VGX-1027

VGX-1027 is a potent immunomodulatory agent [1].

Immunotherapy refers to treatment of disease by suppressing, inducing or enhancing an immune response.

VGX-1027 is an isoxazoline compound with potent immunomodulatory properties [1]. In microarray analysis, VGX-1027 modulated the expression of genes that involved in immune activation and the antigen processing and presentation in response to lipopolysaccharide (LPS) stimulation [2]. In CD4+CD25− T cells, VGX-1027 inhibited cell proliferation induced by enterobacterial antigen [3].

In NOD mice with spontaneous or accelerated diabetes, VGX-1027 significantly reduced the incidence of insulitis and diabetes. In CBA/H mice, VGX-1027 significantly inhibited the development of hyperglycemia and destructive insulitis induced by multiple low doses of streptozotocin. Also, VGX-1027 inhibited the production of inducible nitric-oxide synthase-mediated nitric oxide, macrophage migration inhibitory factor, proinflammatory mediators tumor necrosis factor-α and IL-1β in pancreatic islets [1]. In NZB/NZW F1 mice with systemic lupus erythematosus (SLE), VGX-1027 ameliorated the disease and increased survival [2]. In mice with acute inflammatory colitis, VGX-1027 inhibited the development of colitis. Also, VGX-1027 reduced the production of proinflammatory cytokines TNF-α, IL-12p70, interleukin (IL)-1β, interferon (IFN)-γ and nuclear factor NF-κB (p65) [3].

References:
[1].  Stosic-Grujicic S, Cvetkovic I, Mangano K, 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, 320(3): 1038-1049.
[2].  Fagone P, Muthumani K, Mangano K, et al. VGX-1027 modulates genes involved in lipopolysaccharide-induced Toll-like receptor 4 activation and in a murine model of systemic lupus erythematosus. Immunology, 2014, 142(4): 594-602.
[3].  Mangano K, Sardesai N, D'Alcamo M, et al. In vitro inhibition of enterobacteria-reactive CD4+CD25- T cells and suppression of immunoinflammatory colitis in mice by the novel immunomodulatory agent VGX-1027. Eur J Pharmacol, 2008, 586(1-3): 313-321.

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References on VGX-1027

Effects of the immunomodulator, VGX-1027, in endotoxin-induced uveitis in Lewis rats.[Pubmed:18776919]

Br J Pharmacol. 2008 Nov;155(5):722-30.

BACKGROUND AND PURPOSE: VGX-1027 is a novel, low molecular weight, immunomodulatory compound that has shown efficacy against a variety of immuno-inflammatory disease models in animals including autoimmune diabetes in NOD mice, collagen-induced arthritis and chemically induced inflammatory colitis. Here, we have studied the effects of VGX-1027 on the development of endotoxin-induced uveitis (EIU) in male Lewis rats, as a model of inflammatory ocular diseases in humans. EXPERIMENTAL APPROACH: EIU was induced by a single footpad injection of 200 microg lipopolysaccharide (LPS). Groups of rats were treated with either VGX-1027 (25 mg kg(-1)) or its vehicle at different time points (30 min, 6 h or 12 h) after the challenge with LPS or, as positive control, with dexamethasone. The rats were killed within 16 h after LPS challenge, and the eyes and aqueous humor were collected to study serological, immunological and histological signs of EIU. KEY RESULTS: The rats treated with VGX-1027 within 6 h after LPS challenge exhibited milder clinical, histological and laboratory signs of EIU than those treated with vehicle. CONCLUSION AND IMPLICATIONS: This study provides the first evidence that systemic treatment with VGX-1027 counteracts the uveitis-inducing effect of LPS in rats and suggests that this drug may have potential in the treatment of immuno-inflammatory conditions of the eye in humans.

VGX-1027 modulates genes involved in lipopolysaccharide-induced Toll-like receptor 4 activation and in a murine model of systemic lupus erythematosus.[Pubmed:24527796]

Immunology. 2014 Aug;142(4):594-602.

VGX-1027 [(S,R)-3-phenyl-4,5-dihydro-5-isoxasole acetic acid] is a small molecule compound with immunomodulatory properties, which favourably influences the development of immuno-inflammatory and autoimmune diseases in different animal models such as type 1 diabetes mellitus, pleurisy, rheumatoid arthritis and inflammatory bowel disease. However, the precise mechanism of action of VGX-1027 remains to be ascertained. With this aim, we have studied the immunomodulatory effects of VGX-1027 in vitro, using a genome-wide oligonucleotide microarray approach, and in vivo, using the NZB/NZW F1 model of systemic lupus erythematosus. Microarray data revealed that the administration of VGX-1027 profoundly affected the immune response to exogenous antigens, by modulating the expression of genes that are primarily involved in antigen processing and presentation as well as genes that regulate immune activation. When administered in vivo VGX-1027 ameliorated the course of the disease in the NZB/NZW F1 mice, which correlated with higher per cent survival and improved clinical and histopathological signs. The data presented herein support the theory that VGX-1027 modulates immunity, probably by inhibiting inflammatory antigen presentation and so limiting immune cell expansion.

Safety, bioavailability, and pharmacokinetics of VGX-1027-A novel oral anti-inflammatory drug in healthy human subjects.[Pubmed:27138022]

Clin Pharmacol Drug Dev. 2016 Mar;5(2):91-101.

VGX-1027, a novel oral immune modulator, is under development for the treatment of rheumatoid arthritis. The safety, tolerability, and pharmacokinetics of single (1-800 mg) and multiple (40-400 mg) oral doses were evaluated in 2 clinical studies. The doses were well tolerated up to 800 mg in a single dose and 200 mg twice daily in multiple doses. Adverse events were mild to moderate in severity with no identifiable dose-related pattern. There were no clinically significant physical or laboratory findings. The pharmacokinetic data indicated that increases in Cmax and AUC0-inf were dose-proportional, and AUC0- tau was approximately dose-proportional. For the single-dose study, median Tmax ranged from 0.5 to 2 hours and mean t1/2 ranged from 4.9 to 8.7 hours. For the multiple-dose study, median Tmax ranged from 0.5 to 2.0 hours and mean t1/2 ranged from 7.05 to 10.05 hours. No accumulation of the drug was observed after day 1, indicating that steady-state concentrations were attained with single and multiple dosing for 5 days. Approximately 90% of the administered dose was excreted in urine as unchanged drug.

In vitro inhibition of enterobacteria-reactive CD4+CD25- T cells and suppression of immunoinflammatory colitis in mice by the novel immunomodulatory agent VGX-1027.[Pubmed:18374912]

Eur J Pharmacol. 2008 May 31;586(1-3):313-21.

VGX-1027 is an isozaxoline compound that has recently been found to primarily target the function of murine macrophages but not of T cells, inhibiting secretion of tumor necrosis factor (TNF)-alpha in response to different Toll-like receptor agonists in vitro and in vivo. The well-defined role of innate immunity in inflammatory bowel diseases prompted us to consider the use of VGX-1027 in these diseases leading us to in vitro and in vivo test the drug in related experimental conditions. These consist, respectively, of the proliferation assay of CD4+CD25- T cells to enterobacteria, and the acute inflammatory colitis induced in mice by intracolonic challenge with dinitrobenzene sulfonic acid. The data from the two sets of experiments revealed that VGX-1027 inhibited both proliferation of enterobacterial antigen-reactive CD4+CD25- T cells in vitro and the development of clinical and histological signs of colitis in vivo. The beneficial effect in this model was associated with reduced colonic production of proinflammatory cytokines such as interleukin (IL)-1beta, TNF-alpha, IL-12p70 and interferon (IFN)-gamma and lower content of nuclear factor (NF)-kappaB (p65). These findings seem to warrant investigations of VGX-1027 for use in human.

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.[Pubmed:17449326]

Clin Immunol. 2007 Jun;123(3):311-23.

We have presently studied the in vitro, ex vivo and in vivo immunopharmacological effects of VGX-1027 [(S,R)-3-phenyl-4,5-dihydro-5-isoxasole acetic acid]. This compound reduced the secretion of IL-1beta, TNF-alpha and IL-10 from purified murine macrophages stimulated "in vitro" with lipopolysaccharide (LPS), and it also modified the signaling pathways induced in these cells by LPS entailing reduced activation of NF-kappaB and p38 MAP kinase pathways along with up-regulation of ERK pathways. VGX-1027 appeared to spare T cell function as it was unable to modify the proliferation and/or secretion of IL-2, IFN-gamma and IL-4 induced in purified murine CD4+ T cells from stimulation with either CD3+CD28 or ConA. These effects on macrophages may account for the capacity of VGX-1027 to markedly ameliorate the course of both acute and chronic immunoinflammatory diseases in mice such as carrageenan-induced pleurisy, LPS-induced lethality and type II collagen-induced arthritis. Acute and subacute toxicological studies show that the drug is not toxic at the doses that exert biological effects in these preclinical models. These data warrant additional studies for the potential use of VGX-1027 in the clinical setting.

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.[Pubmed:17148780]

J Pharmacol Exp Ther. 2007 Mar;320(3):1038-49.

(S,R)-3-Phenyl-4,5-dihydro-5-isoxasole acetic acid (VGX-1027) is an isoxazole compound that exhibits various immunomodulatory properties. The capacity of VGX-1027 to prevent interleukin (IL)-1beta plus interferon-gamma-induced pancreatic islet death in vitro prompted us to evaluate its effects on the development of autoimmune diabetes in preclinical models of human type 1 diabetes mellitus (T1D). Administration of VGX-1027 to NOD mice with spontaneous or accelerated forms of diabetes induced either by injection of cyclophosphamide or by transfer of spleen cells from acutely diabetic syngeneic donors markedly reduced the cumulative incidence of diabetes and insulitis. In addition, VGX-1027 given either i.p. or p.o. to CBA/H mice made diabetic with multiple low doses of streptozotocin successfully counteracted the development of destructive insulitis and hyperglycemia. The animals receiving VGX-1027 exhibited reduced production of the proinflammatory mediators tumor necrosis factor-alpha, IL-1beta, macrophage migration inhibitory factor, and inducible nitric-oxide synthase-mediated nitric oxide generation in both pancreatic islets and peripheral compartments. These results indicate that VGX-1027 probably exerts its antidiabetogenic effects by limiting cytokine-mediated immunoinflammatory events, leading to inflammation and destruction of pancreatic islets. VGX-1027 seems worthy of being considered as a candidate drug in the development of new therapeutic strategies for the prevention and early treatment of T1D.

Description

VGX-1027(GIT27) is an isoxazole compound that exhibits various immunomodulatory properties; reduce the secretion of IL-1beta, TNF-alpha and IL-10 from purified murine macrophages.

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