| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
αvβ3 α5β1 αIIbβ3
Integrins alphaIIbbeta3, alphavbeta3, and alpha5beta1; functions as a potent antagonist, blocking integrin-mediated cell adhesion, platelet aggregation, and osteoclast-mediated bone resorption. |
|---|---|
| ln Vitro |
Echistatin TFA is a potent inhibitor of platelet aggregation, with an IC50 in the low nanomolar range (0.1-1 nM) against alphaIIbbeta3. It also potently inhibits bone resorption in culture (osteoclast assays) and blocks cell adhesion to vitronectin and fibronectin by antagonizing alphavbeta3 and alpha5beta1 integrins.
|
| ln Vivo |
Echistatin TFA inhibits platelet aggregation in vivo when administered intravenously in animal models. It has been shown to inhibit tumor cell metastasis and angiogenesis by blocking integrin-mediated cell adhesion and migration in murine models.
|
| Enzyme Assay |
Integrin binding affinity is assessed by competitive ELISA: microtiter plates are coated with purified alphaIIbbeta3, alphavbeta3, or alpha5beta1; Echistatin (0.001-100 nM) competes with biotinylated fibronectin or vitronectin; binding is detected with streptavidin-HRP. IC50 values are determined from displacement curves.
|
| Cell Assay |
Human platelets or HUVEC cells are pre-incubated with Echistatin TFA (0.1-100 nM) for 15-30 min; platelet aggregation is induced by ADP or thrombin and measured by aggregometry; osteoclasts are cultured on bone slices with Echistatin; resorption pits are visualized by toluidine blue staining.
|
| Animal Protocol |
Mice are injected intravenously with Echistatin TFA (0.1-1 mg/kg) 10-15 min before tumor cell injection in metastasis models. Platelet aggregation is measured by bleeding time; tumor cell adhesion to endothelium is assessed by intravital microscopy; lung metastasis colonies are counted.
|
| ADME/Pharmacokinetics |
Not applicable; as a disintegrin peptide, Echistatin TFA has a very short plasma half-life (minutes) due to rapid renal clearance and proteolytic degradation. It is typically used in acute ex vivo and in vivo studies rather than as a therapeutic.
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| Toxicity/Toxicokinetics |
No dedicated toxicity data for the TFA salt. Snake venom disintegrins at high doses can cause bleeding diathesis due to platelet aggregation inhibition. At research doses, toxicity is minimal. For research use only, not for human administration.
|
| References |
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| Additional Infomation |
Echistatin TFA is a research-grade tool for studying integrin biology, platelet aggregation, bone resorption, angiogenesis, and tumor metastasis. It has no clinical trial status or marketing approval as a therapeutic agent. For research use only.
|
| Molecular Formula |
C219H342F3N71O76S9
|
|---|---|
| Molecular Weight |
5531.02
|
| Related CAS # |
Echistatin;154303-05-6
|
| Appearance |
White to off-white solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O :~50 mg/mL (~9.04 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (9.04 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.1808 mL | 0.9040 mL | 1.8080 mL | |
| 5 mM | 0.0362 mL | 0.1808 mL | 0.3616 mL | |
| 10 mM | 0.0181 mL | 0.0904 mL | 0.1808 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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