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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product NameWX-671/Mesupron
SynonymsWX-671
CAS590368-25-5
EINECS
Chemical FormulaC32H47N5O6S
Molecular Weight629.81048
inchi
Package10 mM * 1 mL;1 mg;5 mg;10 mg
PriceEmail to quote
DescriptionsUpamostat

Upamostat

MedChemExpress (MCE)

HY-16511

590368-25-5

WX-671

99.02%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Room temperature in continental US

Descriptions

Upamostat

Upamostat

MedChemExpress (MCE)

HY-16511

590368-25-5

WX-671

99.02%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Room temperature in continental US
may vary elsewhere.

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.

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].

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].

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].

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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Upamostat Related Antibodies

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[1]. Heinemann V, et al. Phase II randomised proof-of-concept study of the urokinase inhibitor upamostat (WX-671) in combination with gemcitabine compared with gemcitabine alone in patients with non-resectable, locally advanced pancreatic cancer. Br J Cancer. 2013 Mar 5
108(4):766-70.
[Content Brief]

[2]. Froriep D, et al. Activation of the anti-cancer agent upamostat by the mARC enzyme system. Xenobiotica. 2013 Sep
43(9):780-4.
[Content Brief]

[3]. Park C, et al. HPLC-MS/MS analysis of mesupron and its application to a pharmacokinetic study in rats. J Pharm Biomed Anal. 2018 Feb 20
150:39-42.
[Content Brief]

Supplier Websitehttps://www.medchemexpress.com/Upamostat.html
Last Update2025-05-21 16:50:25
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