Zalunfiban (RUC-4) di-HCl is a potent and specific platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban di-HCl may be utilized in the study of myocardial infarction.

Physicochemical Properties

Molecular Formula	C16H20CL2N8O2S
Molecular Weight	459.35
CAS #	2815778-41-5
Related CAS #	Zalunfiban;1448313-27-6
Appearance	Light yellow to green yellow 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)

Biological Activity

Targets	IC50: 45 nM (αIIbβ3)[1]
ln Vivo	Platelet aggregation occurs when zalunfiban dihydrochloride (1~3.86 mg/kg; sc; 24 hours) is administered[1]. High-grade suppression of platelet aggregation is initiated within 15–30 minutes by Zalunfiban dihydrochloride (1~3.86 mg/kg; im; 4.5 hours), and it lasts from ~2 to >4.5 hours in a dose-dependent manner[1].
Animal Protocol	Animal/Disease Models: Cynomolgus Monkey Doses: 1~ 3.86 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Sc; 24 hrs (hours) Experimental Results: Platelet aggregation was performed.
References	[1]. Preclinical Studies of RUC-4, a Novel Platelet αIIbβ3 Antagonist, in Non-Human Primates and With Human Platelets. J Clin Transl Sci. 2019;3(2-3):65-74.

Solubility Data

Solubility (In Vitro)

DMSO :~6.67 mg/mL (~14.52 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 0.67 mg/mL (1.46 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 6.7 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: ≥ 0.67 mg/mL (1.46 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 6.7 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. Solubility in Formulation 3: ≥ 0.67 mg/mL (1.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 6.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1770 mL	10.8849 mL	21.7699 mL
	5 mM	0.4354 mL	2.1770 mL	4.3540 mL
	10 mM	0.2177 mL	1.0885 mL	2.1770 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.