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Purity: ≥98%
VGX-1027 (also known as VGX1027; GIT-27) is an orally bioactive, isoxazoline compound with potent immunomodulatory properties by inhibiting the toll-like receptor 4 (TLR4) signaling pathway. By reducing the cytotoxic effects of the cytokines, VGX-1027 significantly reduces IIL-1β/IFN-γ-induced TNF-α and nitrite accumulation and increases cell survival. When lipopolysaccharide (LPS) stimulation was used, the microarray analysis showed that VGX-1027 altered the expression of genes involved in immune activation, antigen processing, and presentation.
| Targets |
IL-1β; IL-10
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| ln Vitro |
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].
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| ln Vivo |
VGX-1027 effectively prevents the onset of destructive insulitis and hyperglycemia (10, 20 mg/kg of i.p. for 12 day or 100 mg/kg of p.o. for 11 day) [1]. In eight-week-old male Lewis rats (180-220 g), VGX-1027 (25 mg/kg; ip; single dose) blocks LPS's ability to cause uveitis[3].
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| Cell Assay |
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. In CD4+CD25− T cells, VGX-1027 inhibited cell proliferation induced by enterobacterial antigen.
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| References |
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| Molecular Formula |
C11H11NO3
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| Molecular Weight |
205.21
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| Exact Mass |
205.07389
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| Elemental Analysis |
C, 64.38; H, 5.40; N, 6.83; O, 23.39
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| CAS # |
6501-72-0
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| Appearance |
Solid powder
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| SMILES |
C1C(ON=C1C2=CC=CC=C2)CC(=O)O
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| InChi Key |
MUFJHYRCIHHATF-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-(3-phenyl-4,5-dihydro-1,2-oxazol-5-yl)acetic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (12.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO +30%PEG 300 +5% Tween 80 +ddH2O: 10mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8731 mL | 24.3653 mL | 48.7306 mL | |
| 5 mM | 0.9746 mL | 4.8731 mL | 9.7461 mL | |
| 10 mM | 0.4873 mL | 2.4365 mL | 4.8731 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00627120 | Completed | Drug: VGX-1027 | Healthy | VGX Pharmaceuticals, LLC | February 2008 | Phase 1 |
| NCT00760396 | Completed | Drug: VGX-1027 | Healthy | VGX Pharmaceuticals, LLC | February 2008 | Phase 1 |
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Products are for research use only; We do not sell to patients
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