| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
The primary targets of Oglufanide include HCV (hepatitis C virus) and VEGFR (vascular endothelial growth factor receptor). It acts as an immunomodulator, stimulating the immune response to HCV and intracellular bacterial infections. It also inhibits VEGF, which contributes to its antitumor and anti-angiogenic activities.
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| ln Vitro |
The chorioallantoic membrane experiment demonstrates a dependent angiogenesis inhibitory action of oglufanide (IM862) (1-1000 μg/mL), which totally inhibits β-FGF and VEGF-induced angiogenesis [3]. -L-trp) (0-1000 μg/mL; 5 days) failed to affect the viability of HUVEC or tumor cells. [4]
In vitro, Oglufanide stimulates immune responses to HCV and intracellular bacterial infections. It inhibits VEGF. Its immunomodulatory activity is typically measured using assays that assess cytokine production, T cell proliferation, or natural killer cell activity. Its anti-angiogenic activity is assessed using endothelial cell proliferation or tube formation assays. |
| ln Vivo |
Oglufanide (L-glu-L-trp) shows anticancer efficacy in vaccines for immunocompetent and immunodeficient individuals (1–100 mg/kg/day; sc; 10 days) [4].
In vivo, Oglufanide has antitumor and anti-angiogenic activities. It stimulates the immune response to HCV and intracellular bacterial infections. It is being developed for the treatment of chronic hepatitis C virus infection. Its efficacy in animal models of HCV infection and cancer has been demonstrated. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Oglufanide are not typically performed, as it acts as an immunomodulator rather than a direct enzyme inhibitor. Its activity is assessed in cell-based assays that measure immune responses. VEGF inhibition can be measured using ELISA or other immunoassays.
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| Cell Assay |
In vitro cellular assays for Oglufanide are conducted in immune cells (e.g., T cells, NK cells) or endothelial cells. Immune cells are treated with the compound, and cytokine production, proliferation, or cytotoxicity is measured. Endothelial cells are treated with the compound, and VEGF-induced proliferation or tube formation is assessed.
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| Animal Protocol |
Animal/Disease Models: C57BL/6 immunocompetent mice, Lewis lung cancer (LLC) xenografts; Balb/C athymic mice, M21 human melanoma xenografts [4] Doses: 1, 10, 50 and 100 mg/ kg/day
Doses: SC, 10 days Experimental Results: Dose-dependent inhibition of LLC tumor growth in syngeneic immunization Xenograft tumor volume in Balb/C athymic mice transplanted with M21 human melanoma cells as a function of dose diminished dependence. In vivo animal studies for Oglufanide are conducted in animal models of HCV infection, cancer, or bacterial infection. Animals are administered the compound orally or intraperitoneally, and viral load, tumor growth, or bacterial burden is measured. Immune responses are assessed by measuring cytokine levels and immune cell populations. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Oglufanide indicate it has a molecular weight of 333.34 and a molecular formula of C16H19N3O5. It is a dipeptide. Its bioavailability and other PK parameters would be determined in preclinical studies. The compound is typically stored at 2-8°C in a dark, inert atmosphere.
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| Toxicity/Toxicokinetics |
Toxicological information for Oglufanide is derived from preclinical studies. As an immunomodulator, it may have effects on immune function. Comprehensive toxicology studies would be required for clinical development, including assessments of its effects on autoimmunity and infection susceptibility.
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| References | |
| Additional Infomation |
Glu-Trp is a dipeptide composed of L-glutamate and L-tryptophan linked by peptide bonds. It has multiple functions, including as a metabolite, immunomodulator, angiogenesis regulator, and antitumor agent. Its functions are related to L-glutamate and L-tryptophan.
Oglufanib is a synthetic dipeptide immunomodulator being developed for the treatment of chronic hepatitis C virus infection. Oglufanib was initially developed in Russia (registered as a drug there) for the treatment of serious infectious diseases and underwent extensive cancer clinical trials in the United States before being acquired by Implicit Bioscience in 2005. Oglufanib is administered intranasally as an immunomodulator for the treatment of patients with chronic hepatitis C virus infection. Pharmacodynamics Oglufanib works by modulating the body's inherent immune response to fight invading pathogens and cancer cells. It may control or reverse the immune system suppression utilized by hepatitis viruses, thereby opposing our normal healthy defense mechanisms. Oglufanide is a dipeptide immunomodulator being developed for the treatment of chronic hepatitis C virus infection. It is also known as H-Glu-Trp-OH. It stimulates immune responses to HCV and intracellular bacterial infections and has antitumor and anti-angiogenic activities. It is available from research chemical suppliers for preclinical studies. It is not approved for clinical use. |
| Molecular Formula |
C16H19N3O5
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|---|---|
| Molecular Weight |
333.3392
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| Exact Mass |
333.132
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| CAS # |
38101-59-6
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| PubChem CID |
100094
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
738.9±60.0 °C at 760 mmHg
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| Flash Point |
400.7±32.9 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.659
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| LogP |
0.5
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
24
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| Complexity |
484
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1=CC=C2C(=C1)C(=CN2)C[C@@H](C(=O)O)NC(=O)[C@H](CCC(=O)O)N
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| InChi Key |
LLEUXCDZPQOJMY-AAEUAGOBSA-N
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| InChi Code |
InChI=1S/C16H19N3O5/c17-11(5-6-14(20)21)15(22)19-13(16(23)24)7-9-8-18-12-4-2-1-3-10(9)12/h1-4,8,11,13,18H,5-7,17H2,(H,19,22)(H,20,21)(H,23,24)/t11-,13-/m0/s1
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| Chemical Name |
(4S)-4-amino-5-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-5-oxopentanoic acid
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~15.5 mg/mL (~46.50 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.50 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 (7.50 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 (7.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9999 mL | 14.9997 mL | 29.9994 mL | |
| 5 mM | 0.6000 mL | 2.9999 mL | 5.9999 mL | |
| 10 mM | 0.3000 mL | 1.5000 mL | 2.9999 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.
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