| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary biological target of glufanide disodium is not fully defined. It is classified as an immunomodulator and angiogenesis inhibitor. Its mechanism is believed to involve modulation of cytokine production and immune cell function, potentially through interactions with immune receptors or intracellular signaling pathways. Angiogenesis inhibition may be mediated through interference with endothelial cell proliferation and migration, though specific molecular targets remain under investigation.
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|---|---|
| ln Vitro |
In vitro studies have evaluated glufanide disodium for its immunomodulatory and antiangiogenic properties. It has been shown to inhibit endothelial cell proliferation and tube formation in Matrigel assays. Immunomodulatory effects include enhancement of natural killer cell activity and modulation of cytokine release from peripheral blood mononuclear cells. Specific IC50 values have not been consistently reported across studies.
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| ln Vivo |
In vivo, glufanide disodium has demonstrated activity in animal models of angiogenesis and viral infection. In tumor xenograft models, it inhibited neovascularization and tumor growth. In viral infection models, it enhanced host immune responses. Clinical trials in hepatitis C patients showed limited efficacy as monotherapy. Pharmacokinetic studies indicate rapid clearance following intravenous administration.
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| Enzyme Assay |
Receptor binding assays for glufanide disodium have not been extensively characterized due to its undefined molecular target. General non-cell-based protocols for immunomodulatory peptides involve radioligand binding assays using membrane preparations from immune cells or endothelial cells. Competition binding experiments with labeled cytokines or growth factors can assess potential receptor interactions.
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| Cell Assay |
Cell-based assays for glufanide disodium include proliferation assays using human umbilical vein endothelial cells (HUVECs) and immune cell functional assays. HUVECs are cultured in endothelial growth medium and treated with test compound; proliferation is measured by BrdU incorporation or MTT assay. Tube formation assays on Matrigel are used to assess angiogenic activity.
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| Animal Protocol |
In vivo animal protocols for glufanide disodium typically use murine tumor models or viral infection models. Mice receive intravenous or subcutaneous administration at doses ranging from 1-30 mg/kg. Tumor growth is monitored by caliper measurement. Immunological parameters such as NK cell cytotoxicity and cytokine levels are assessed from splenocytes and serum samples.
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| References | |
| Additional Infomation |
Oglufanide disodium is the synthetic disodium salt of a naturally occurring dipeptide (composed of L-glutamic acid and L-tryptophan) with potential anti-angiogenic and immunomodulatory activities. Oglufanide inhibits vascular endothelial growth factor (VEGF), thereby suppressing angiogenesis. It has also been reported to stimulate the body's immune response to hepatitis C virus and intracellular bacterial infections.
See also: Oglufanide (note moved to). |
| Molecular Formula |
C16H17N3NA2O5
|
|---|---|
| Molecular Weight |
377.3
|
| Exact Mass |
377.096
|
| CAS # |
237068-57-4
|
| PubChem CID |
158780
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
738.9ºC at 760mmHg
|
| Flash Point |
400.7ºC
|
| Vapour Pressure |
6.29E-23mmHg at 25°C
|
| LogP |
0.55
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
473
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O=C(O)[C@@H](NC([C@@H](N)CCC(O)=O)=O)CC1=CNC2=CC=CC=C21.[Na].[Na].[H].[H]
|
| InChi Key |
GDLPAGOVHZLZEK-JBUFHSOLSA-L
|
| InChi Code |
InChI=1S/C16H19N3O5.2Na/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);;/q;2*+1/p-2/t11-,13-;;/m0../s1
|
| Chemical Name |
disodium;(4S)-4-amino-5-[[(1S)-1-carboxylato-2-(1H-indol-3-yl)ethyl]amino]-5-oxopentanoate
|
| Synonyms |
IM 862; IM862; Glufanide disodium
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6504 mL | 13.2521 mL | 26.5041 mL | |
| 5 mM | 0.5301 mL | 2.6504 mL | 5.3008 mL | |
| 10 mM | 0.2650 mL | 1.3252 mL | 2.6504 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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