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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%
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.

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

Tirofiban hydrochloride monohydrate Chemical Structure

Tirofiban hydrochloride monohydrate Chemical Structure

CAS No. : 150915-40-5

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Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 86 In-stock
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50 mg USD 290 In-stock
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100 mg USD 528 In-stock
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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].

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].

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.
SMILES

O=S(N[[email protected]](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)

H2O : 1 mg/mL (2.02 mM; Need ultrasonic)

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
10 mM 0.2020 mL 1.0100 mL 2.0199 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.34%

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Tirofiban hydrochloride monohydrate
Cat. No.:
HY-17369
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