| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 500mg |
| Targets |
RUC-4 selectively targets the αIIbβ3 integrin (also known as glycoprotein IIb/IIIa), a receptor on the surface of platelets that mediates platelet aggregation. By binding to αIIbβ3, RUC-4 prevents the cross-linking of platelets by fibrinogen, thereby inhibiting platelet aggregation. Its non-RGD-mimetic nature means it does not mimic the arginine-glycine-aspartic acid (RGD) sequence found in natural ligands, potentially offering a different binding profile and reduced immunogenicity. It shows no activity on αVβ3 receptors, indicating high selectivity.
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| ln Vitro |
In vitro, RUC-4 is a potent antagonist of αIIbβ3 with an IC50 of 45 nM. It inhibits platelet aggregation in a dose-dependent manner. The compound's selectivity for αIIbβ3 over αVβ3 makes it a valuable tool for studying platelet-specific functions without off-target effects on other integrins. In platelet aggregation assays, RUC-4 effectively blocks fibrinogen binding and subsequent platelet clumping, confirming its mechanism of action as a platelet aggregation inhibitor.
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| ln Vivo |
Platelet aggregation is a side effect of zelunfiban (1~3.86 mg/kg; sc; 24 hours) [1]. Within 15 to 30 minutes, zalunfiban (1~3.86 mg/kg; IM; 4.5 hours) induces a high degree of platelet aggregation inhibition that lasts for around 2 to >4.5 hours in a dose-dependent manner [1].
In vivo, RUC-4 has been studied for prehospital therapy of myocardial infarction. In cynomolgus monkeys, subcutaneous administration of zalunfiban (RUC-4) at 1-3.86 mg/kg induces a high degree of platelet aggregation inhibition within 15 to 30 minutes that lasts for around 2 to >4.5 hours in a dose-dependent manner. This rapid onset and sustained effect make it suitable for acute settings such as prehospital MI treatment. The compound is administered via subcutaneous or intramuscular injection. |
| Enzyme Assay |
Non-cellular in vitro assays for RUC-4 involve receptor binding studies using purified αIIbβ3 integrin. A standard protocol uses a competitive binding assay with a labeled ligand (e.g., biotinylated fibrinogen or a specific peptide) that binds to the αIIbβ3 receptor. Varying concentrations of RUC-4 are incubated with the receptor and the labeled ligand. After incubation, the bound ligand is captured on a solid phase (e.g., streptavidin-coated plates), and the signal is measured. The IC50 is determined from the inhibition curve.
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| Cell Assay |
Cellular assays for RUC-4 are performed using human platelets. Platelet-rich plasma (PRP) is prepared from whole blood. RUC-4 is added to the PRP at various concentrations and pre-incubated for a short period. Platelet aggregation is induced by the addition of an agonist such as ADP, thrombin, or collagen. The aggregation is measured using a platelet aggregometer, which monitors the increase in light transmission as platelets aggregate. The IC50 for inhibition of aggregation is determined.
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| Animal Protocol |
Animal/Disease Models: Cynomolgus monkey
Doses: 1~3.86 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Sc; 24-hour Experimental Results: Platelet aggregation. In vivo animal studies for RUC-4 are conducted in cynomolgus monkeys. Animals are administered RUC-4 via subcutaneous or intramuscular injection at doses of 1-3.86 mg/kg. Blood samples are collected at various time points post-administration. Platelet aggregation is measured ex vivo using platelet aggregometry. The degree and duration of platelet inhibition are determined. Pharmacokinetic parameters are also assessed from the blood samples. |
| ADME/Pharmacokinetics |
RUC-4 has a molecular weight of 386.43 and is soluble in DMSO at ~17.86 mg/mL. For in vivo studies, it can be formulated in 10% DMSO, 40% PEG300, 5% Tween-80, and 45% Saline. The compound has a logP of -1.2, indicating high hydrophilicity. It is administered via subcutaneous or intramuscular injection for rapid onset of action. Pharmacokinetic studies in cynomolgus monkeys have been conducted, though detailed parameters are not provided in the available literature.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for RUC-4 have not been extensively reported. As a research chemical, it is not intended for human use and is strictly for preclinical research purposes. Standard safety precautions should be followed when handling RUC-4, including the use of personal protective equipment. The compound is typically stored as a powder at -20°C for up to three years or at 4°C for up to two years. No specific toxicity data, such as LD50 values, are available in the provided literature.
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| References | |
| Additional Infomation |
RUC-4 (Zalunfiban) is a potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist. It is being investigated for prehospital therapy of myocardial infarction due to its rapid onset of action and high potency. The compound is administered subcutaneously or intramuscularly, making it suitable for use in emergency settings by first responders. RUC-4 is not a clinically approved drug but has been studied in preclinical models. Its primary application is in cardiovascular research.
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| Molecular Formula |
C16H18N8O2S
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|---|---|
| Molecular Weight |
386.431519985199
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| Exact Mass |
386.127
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| CAS # |
1448313-27-6
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| Related CAS # |
Zalunfiban dihydrochloride
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| PubChem CID |
71668132
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-1.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
715
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YTFMOSCBEAMELI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H18N8O2S/c17-9-13(25)20-11-7-10(1-2-19-11)15-22-24-14(26)8-12(21-16(24)27-15)23-5-3-18-4-6-23/h1-2,7-8,18H,3-6,9,17H2,(H,19,20,25)
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| Chemical Name |
2-Amino-N-[5-[5-oxo-7-(1-piperazinyl)-5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-2-yl]-3-pyridinyl]acetamide
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| Synonyms |
RUC-4 RUC 4 RUC4
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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 |
| 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 : ~17.86 mg/mL (~46.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.38 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 20.8 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: ≥ 2.08 mg/mL (5.38 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 20.8 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: ≥ 2.08 mg/mL (5.38 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 | 2.5878 mL | 12.9390 mL | 25.8779 mL | |
| 5 mM | 0.5176 mL | 2.5878 mL | 5.1756 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5878 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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