| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Glycoprotein GPⅡb/Ⅲa
Batifiban TFA targets the platelet glycoprotein GPIIb/IIIa (integrin alphaIIbbeta3), the primary receptor for fibrinogen and von Willebrand factor on activated platelets. It also blocks the binding of circulating vitronectin to integrin alphaνbeta3, thereby inhibiting platelet aggregation and thrombus formation. |
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| ln Vitro |
In cell‑free assays, Batifiban TFA selectively binds to purified GPIIb/IIIa with high affinity, blocking the interaction with fibrinogen and vitronectin. The peptide has good water solubility due to its TFA salt form, facilitating its use in a variety of assay systems.
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| ln Vivo |
In vivo, Batifiban TFA inhibits platelet aggregation and reduces thrombus formation in animal models of arterial thrombosis. By blocking the GPIIb/IIIa receptor on activated platelets, it prevents cross‑linking of platelets via fibrinogen, thereby reducing the risk of occlusive thrombus formation.
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| Enzyme Assay |
A standard in vitro receptor binding protocol: Purified human GPIIb/IIIa (integrin alphaIIbbeta3) is immobilised on a 96‑well plate. Batifiban TFA is added at 0.1 nM‑10 uM, followed by biotinylated fibrinogen (1 ug/mL). After washing, bound fibrinogen is detected with streptavidin‑HRP and substrate. IC50 values are calculated from inhibition curves.
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| Cell Assay |
A general in vitro platelet aggregation assay: Human platelet-rich plasma (PRP) is prepared by centrifugation. Batifiban TFA (0.1‑100 uM) is added to PRP and incubated for 5 min at 37degC. Aggregation is induced by adding ADP (10 uM) or collagen (2 ug/mL) and monitored using a light transmission aggregometer for 5‑10 min. Results are expressed as percentage inhibition of maximal aggregation.
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| Animal Protocol |
A general in vivo thrombosis model: Male Sprague‑Dawley rats (n=6/group) are administered Batifiban TFA via intravenous bolus (0.1‑3 mg/kg) 10 min before arterial injury. The carotid artery is injured with FeCl3 (15% for 3 min), and blood flow is monitored with a Doppler flow probe for 60 min. Inhibition of thrombosis is determined by the time to occlusion or vessel patency score.
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| ADME/Pharmacokinetics |
As a cyclic peptide with a disulfide bridge, Batifiban TFA is resistant to proteolytic degradation, offering improved pharmacokinetic properties compared to linear RGD peptides. It is suitable for intravenous administration and has a moderate plasma half‑life. The TFA counterion enhances aqueous solubility for formulation.
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| Toxicity/Toxicokinetics |
Batifiban TFA is a research compound with no approved clinical indications. Toxicology studies are limited; however, GPIIb/IIIa antagonists as a class may increase bleeding risk. Peptide‑based inhibitors generally have favourable safety profiles, but full toxicological characterisation is not available for this analogue.
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| References | |
| Additional Infomation |
Batifiban is a cyclic heptapeptide with the sequence {Mpa}‑Arg‑Gly‑Asp‑Trp‑Pro‑Cys‑NH2, where a disulfide bridge connects Mpa1 and Cys7. It belongs to the class of RGD‑mimetic integrin antagonists and is used in cardiovascular research, particularly for evaluating anti‑thrombotic therapies and integrin‑related signalling in vascular biology.
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| Molecular Formula |
C34H47N11O9S2.XC2HF3O2
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|---|---|
| Molecular Weight |
817.94 (free base)
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| Related CAS # |
Batifiban;710312-77-9
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| Appearance |
White to off-white solid powder
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O :~100 mg/mL
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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.) |
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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