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  3. Tirofiban hydrochloride monohydrate

Tirofiban hydrochloride monohydrate  (Synonyms: L700462 hydrochloride monohydrate; MK383 hydrochloride monohydrate)

Cat. No.: HY-17369 Purity: 99.34%
COA Handling Instructions

Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.

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Tirofiban hydrochloride monohydrate Chemical Structure

Tirofiban hydrochloride monohydrate Chemical Structure

CAS No. : 150915-40-5

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Tirofiban hydrochloride monohydrate:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tirofiban hydrochloride monohydrate

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area[1][2][3].

IC50 & Target

Gp IIb/IIIa Receptor[1]

In Vitro

Tirofiban hydrochloride monohydrate (0.25, 1, 3 μg/mL; 72 hours) increases proliferation of HAEC cells[1].
Tirofiban hydrochloride monohydrate (24 hours) closes the scratch of HUVECs migration within 18 hours[1].
Tirofiban hydrochloride monohydrate (0.25, 1 μg/mL; 1 hour) induces production of VEGF after 30 minutes which can stimulates proliferation of endothelial cells[1].

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

Cell Proliferation Assay[1]

Cell Line: HAEC cells
Concentration: 0.25, 1, 3 μg/mL
Incubation Time: 72 hours
Result: Increased proliferation of HAEC cells.

Cell Migration Assay [1]

Cell Line: HUVEC cells
Concentration:
Incubation Time: 24 hours
Result: Stimulated the migratory capacity of endothelial cells.

Western Blot Analysis[1]

Cell Line: HAEC cells
Concentration: 0.05, 0.12, 0.25, 1 μg/mL
Incubation Time: 1 hour
Result: Induced production of VEGF which stimulated proliferation of endothelial cells.
In Vivo

Tirofiban hydrochloride monohydrate (60 μg/kg; i.v.; once) shows activity of increasing contraction force, ventricular compliance, and improving heart function by increasing HR, LVESP, dp/dtmax, and reducing LVEDP[2].
Tirofiban hydrochloride monohydrate (60 μg/kg; i.v.; once) enhances eNOS activity, decreases iNOS activity and reduces area of no-reflow after reperfusion following AMI[2]. Tirofiban hydrochloride monohydrate (50 µg/per; irrigate; once) shows anticoagulant effect with patency rates of 59% at 24 hours after microvascular anastomosis in the crush model[3].

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

Animal Model: Male Sprague-Dawley rats (10 to 15-week-age; 270-330 g)[2].
Dosage: 60 μg/kg
Administration: Intravenous injection; once.
Result: Increased contraction force, ventricular compliance, and improved heart function.
Reduced the size of no-reflow and infarct.
Animal Model: Sprague-Dawley rats (350-400 g; crush injury model)[3]
Dosage: 50 µg/per (50 µg/mL, 1 mL for each)
Administration: Irrigate 1 mL within the vessel lumen (before placement of the last suture); once.
Result: Showed anticoagulant effect with patency rates of 59%.
Clinical Trial
Molecular Weight

495.07

Formula

C22H39ClN2O6S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(N[C@H](C(O)=O)CC1=CC=C(OCCCCC2CCNCC2)C=C1)(CCCC)=O.[H]Cl.[H]O[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (201.99 mM; Need ultrasonic; 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 2.0199 mL 10.0996 mL 20.1992 mL
5 mM 0.4040 mL 2.0199 mL 4.0398 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 99.34%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0199 mL 10.0996 mL 20.1992 mL 50.4979 mL
5 mM 0.4040 mL 2.0199 mL 4.0398 mL 10.0996 mL
10 mM 0.2020 mL 1.0100 mL 2.0199 mL 5.0498 mL
15 mM 0.1347 mL 0.6733 mL 1.3466 mL 3.3665 mL
20 mM 0.1010 mL 0.5050 mL 1.0100 mL 2.5249 mL
25 mM 0.0808 mL 0.4040 mL 0.8080 mL 2.0199 mL
30 mM 0.0673 mL 0.3367 mL 0.6733 mL 1.6833 mL
40 mM 0.0505 mL 0.2525 mL 0.5050 mL 1.2624 mL
50 mM 0.0404 mL 0.2020 mL 0.4040 mL 1.0100 mL
60 mM 0.0337 mL 0.1683 mL 0.3367 mL 0.8416 mL
80 mM 0.0252 mL 0.1262 mL 0.2525 mL 0.6312 mL
100 mM 0.0202 mL 0.1010 mL 0.2020 mL 0.5050 mL
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  • 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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