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Zalunfiban (RUC-4) is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban can be used for the research of myocardial infarction (MI).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Zalunfiban dihydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Zalunfiban Chemical Structure

Zalunfiban Chemical Structure

CAS No. : 1448313-27-6

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Description

Zalunfiban (RUC-4) is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban can be used for the research of myocardial infarction (MI)[1].

IC50 & Target

IC50: 45 nM (αIIbβ3)[1]

In Vivo

Zalunfiban (1~3.86 mg/kg; s.c.; 24 hours) makes platelet aggregation performed[1].
Zalunfiban (1~3.86 mg/kg; i.m.; 4.5 hours) leads to the onset of high-grade inhibition of platelet aggregation within 15-30 minutes that lasted from ~2 to >4.5 hours in a dose dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cynomolgus Monkey
Dosage: 1~3.86 mg/kg (Pharmacokinetic Analysis)
Administration: S.c.; 24 hours
Result: Platelet aggregation was performed.
Clinical Trial
Molecular Weight

386.43

Formula

C16H18N8O2S

CAS No.
SMILES

O=C(NC1=CC(C(S2)=NN(C2=NC(N3CCNCC3)=C4)C4=O)=CN=C1)CN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 17.86 mg/mL (46.22 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table
  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5878 mL 12.9390 mL 25.8779 mL 64.6948 mL
5 mM 0.5176 mL 2.5878 mL 5.1756 mL 12.9390 mL
10 mM 0.2588 mL 1.2939 mL 2.5878 mL 6.4695 mL
15 mM 0.1725 mL 0.8626 mL 1.7252 mL 4.3130 mL
20 mM 0.1294 mL 0.6469 mL 1.2939 mL 3.2347 mL
25 mM 0.1035 mL 0.5176 mL 1.0351 mL 2.5878 mL
30 mM 0.0863 mL 0.4313 mL 0.8626 mL 2.1565 mL
40 mM 0.0647 mL 0.3235 mL 0.6469 mL 1.6174 mL
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Zalunfiban Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Zalunfiban
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