1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease

Upamostat (Synonyms: WX-671)

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

Upamostat 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
100 mg   Get quote  
200 mg   Get quote  

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Description

Upamostat 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].

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].

Clinical Trial
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
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Upamostat
Cat. No.:
HY-16511
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Upamostat

Cat. No.: HY-16511