| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Glycoprotein IIb/IIIa (GPIIb/IIIa) receptor (integrin αIIbβ3) on platelets; fibrinogen.
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| ln Vitro |
Gly-Pro-Arg-Pro Acetate (GPRP) is a fibrin polymerization inhibitor that suppresses the interaction between fibrinogen and the platelet membrane glycoprotein IIb/IIIa complex (glycoprotein IIb/IIIa receptor). By inhibiting this interaction, GPRP prevents platelet aggregation and fibrin clot formation. The peptide mimics the N-terminus of the fibrin α-chain, competing with fibrinogen for binding to the GPIIb/IIIa receptor. Specific IC50 values for inhibition of platelet aggregation are available in the literature. GPRP is a tetrapeptide with the sequence Gly-Pro-Arg-Pro.
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| ln Vivo |
In vivo efficacy of GPRP has been studied in animal models of thrombosis and hemostasis. By inhibiting platelet aggregation and fibrin polymerization, GPRP can prevent thrombus formation. The compound has been used to study the role of the GPIIb/IIIa receptor in thrombosis and to validate this receptor as a target for antithrombotic therapy. Specific dosing regimens and detailed efficacy data are available in the primary literature.
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| Enzyme Assay |
Glycoprotein IIb/IIIa receptor binding is assessed using in vitro binding assays with purified GPIIb/IIIa receptor or with platelets. Competitive binding with fibrinogen or other ligands is measured. Platelet aggregation is assessed using platelet-rich plasma (PRP) and aggregation inducers (e.g., ADP, collagen, thrombin). Inhibition of platelet aggregation is measured in the presence of varying concentrations of GPRP. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular activity is evaluated in platelets. Platelet-rich plasma (PRP) is prepared from blood samples. Platelets are treated with GPRP at various concentrations (typically 0.1-1000 µM) and stimulated with platelet aggregation inducers (e.g., ADP, collagen, thrombin). Platelet aggregation is measured using light transmission aggregometry or impedance aggregometry. Fibrinogen binding to platelets may be assessed by flow cytometry using fluorescently labeled fibrinogen.
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| Animal Protocol |
In vivo efficacy is studied in animal models of thrombosis, such as the ferric chloride-induced arterial thrombosis model or the venous stasis thrombosis model. GPRP is administered via various routes (intravenous, intraperitoneal) at doses determined from pharmacokinetic and tolerability studies. Thrombus formation is assessed by measuring thrombus weight, vessel occlusion, or by using Doppler flow probes. Platelet aggregation is assessed ex vivo. Bleeding time may be measured to assess hemostatic effects.
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| ADME/Pharmacokinetics |
GPRP (Gly-Pro-Arg-Pro Acetate) has a molecular formula of C18H31N7O5 and a molecular weight of 425.49 g/mol. CAS Number: 67869-62-9. Appearance: Solid. Purity: typically ≥98% by HPLC. The compound is a synthetic peptide. Storage: Powder at -20°C for long-term stability. It is soluble in water and DMSO. The compound is typically supplied as the acetate salt.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GPRP are not extensively published. As a research peptide that inhibits platelet aggregation, it may have antithrombotic effects and increase the risk of bleeding. The compound should be handled with appropriate safety precautions. It is for research use only and not for human therapeutic applications without appropriate regulatory approval. Standard laboratory safety practices should be followed, including the use of personal protective equipment and adequate ventilation.
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| References | |
| Additional Infomation |
GPRP (Gly-Pro-Arg-Pro Acetate) is a research tool compound for studying platelet function, hemostasis, and thrombosis. It is not approved for clinical use. The compound is a fibrin polymerization inhibitor that suppresses the interaction between fibrinogen and the platelet membrane glycoprotein IIb/IIIa complex. GPRP is a tetrapeptide that mimics the N-terminus of the fibrin α-chain, competing with fibrinogen for binding to the GPIIb/IIIa receptor. It is used in research to investigate the molecular mechanisms of platelet aggregation and to validate the GPIIb/IIIa receptor as a target for antithrombotic therapy. GPRP is a valuable tool for understanding the role of integrins in hemostasis and thrombosis.
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| Molecular Formula |
C20H35N7O7
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|---|---|
| Molecular Weight |
485.54
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| Exact Mass |
425.239
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| CAS # |
67869-62-9
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| Related CAS # |
GPRP acetate;157009-81-9
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| PubChem CID |
123681
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| Appearance |
White to off-white solid powder
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| Density |
1.55 g/cm3
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| Index of Refraction |
1.691
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| LogP |
-4.7
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
694
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1C[C@H](N(C1)C(=O)CN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)O
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| InChi Key |
WXPZDDCNKXMOMC-AVGNSLFASA-N
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| InChi Code |
InChI=1S/C18H31N7O5/c19-10-14(26)24-8-2-5-12(24)15(27)23-11(4-1-7-22-18(20)21)16(28)25-9-3-6-13(25)17(29)30/h11-13H,1-10,19H2,(H,23,27)(H,29,30)(H4,20,21,22)/t11-,12-,13-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-1-(2-aminoacetyl)pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carboxylic acid
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| Synonyms |
Gly-Pro-Arg-Pro Acetate salt; GPRP; Gly-Pro-Arg-Pro Acetate
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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) |
H2O : ≥ 50 mg/mL (~117.51 mM)
DMSO : ~20.83 mg/mL (~48.96 mM) |
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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 | 2.0596 mL | 10.2978 mL | 20.5956 mL | |
| 5 mM | 0.4119 mL | 2.0596 mL | 4.1191 mL | |
| 10 mM | 0.2060 mL | 1.0298 mL | 2.0596 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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