1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
    PAI-1
  3. Upamostat

Upamostat (Synonyms: WX-671)

Cat. No.: HY-16511 Purity: >98.0%
Handling Instructions

Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.

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

Upamostat Chemical Structure

Upamostat Chemical Structure

CAS No. : 590368-25-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 485 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.

IC50 & Target

Serine protease, uPA[1]

In Vitro

Upamostat is the urokinase plasminogen activator (uPA) inhibitor. Upamostat is the oral pro-drug of the active metabolite WX-UK1, a novel uPA inhibitor[1]. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, which plays a major role in tumor invasion and metastasis. Upamostat is the orally available amidoxime- (i.e. hydroxyamidine-) prodrug of the pharmacologically active form, WX-UK1[2].

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

In Vivo

The validated method is used to evaluate the pharmacokinetics of Upamostat (Mesupron) in rats. The mean plasma concentrations of Upamostat after a single intravenous injection of 2 mg/kg in five rats are measured. The substance decays in a mono-phasic pattern with a terminal half-life of 0.5 h; its volume of distribution is 2.0 L/kg, and clearance is about 2.7 L/h/kg[3].

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

Clinical Trial
Molecular Weight

629.81

Formula

C₃₂H₄₇N₅O₆S

CAS No.

590368-25-5

SMILES

O=C(N1CCN(C([[email protected]@H](NS(=O)(C2=C(C(C)C)C=C(C(C)C)C=C2C(C)C)=O)CC3=CC=CC(C(NO)=N)=C3)=O)CC1)OCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (396.95 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5878 mL 7.9389 mL 15.8778 mL
5 mM 0.3176 mL 1.5878 mL 3.1756 mL
10 mM 0.1588 mL 0.7939 mL 1.5878 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[3]

Rats[3]
Five 9-week old Sprague-Dawley rats are administered a single intravenous injection of 2 mg/kg of Upamostat. Upamostat is dissolved in a mixture of normal saline, dimethylacetamide, polyethylene glycol 400 and DMSO (3:3:3:1). Blood samples (0.15 mL) are taken serially for up to 10 h after drug administration and collected in heparinized centrifuge tubes. After centrifugation at 13,200 rpm for 10 min, the plasma samples are analyzed[3].

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

References
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Keywords:

UpamostatWX-671WX671WX 671Ser/Thr ProteasePAI-1Serine proteasesSerine endopeptidasesThreonine proteasesPlasminogen activator inhibitor-1Inhibitorinhibitorinhibit

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Upamostat
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