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

Upamostat (WX-671), a prodrug of WX-UK1, is an orally active serine protease inhibitor. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, blocking the plasminogen activation process mediated by it, thereby suppressing the invasion, migration and metastasis of tumor cells. Upamostat can be used in the research of metastatic breast cancer and locally advanced pancreatic cancer.

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Upamostat

Upamostat Estructura química

No. CAS : 590368-25-5

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtener un presupuesto  
500 mg   Obtener un presupuesto  

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Based on 1 publication(s) in Google Scholar

Other Forms of Upamostat:

Upamostat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Upamostat

  • Actividad biológica

  • Protocolo

  • Pureza y Documentación

  • Referencias

  • Revisión del cliente

Descripciòn

Upamostat (WX-671), a prodrug of WX-UK1, is an orally active serine protease inhibitor. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, blocking the plasminogen activation process mediated by it, thereby suppressing the invasion, migration and metastasis of tumor cells. Upamostat can be used in the research of metastatic breast cancer and locally advanced pancreatic cancer[1].

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].

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

Upamostat Related Antibodies
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].

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

629.81

Fòrmula

C32H47N5O6S
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C([C@@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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : ≥ 250 mg/mL (396.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculadora de molaridad

  • Calculadora de dilución

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    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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.
Pureza y Documentación

Purity: 99.02%

SDS (544 KB)

COA (251 KB) HNMR (280 KB) LCMS (95 KB)

Instrucciones de manejo (2659 KB)
Referencias
Administraciòn de animales
[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5878 mL 7.9389 mL 15.8778 mL 39.6945 mL
5 mM 0.3176 mL 1.5878 mL 3.1756 mL 7.9389 mL
10 mM 0.1588 mL 0.7939 mL 1.5878 mL 3.9695 mL
15 mM 0.1059 mL 0.5293 mL 1.0585 mL 2.6463 mL
20 mM 0.0794 mL 0.3969 mL 0.7939 mL 1.9847 mL
25 mM 0.0635 mL 0.3176 mL 0.6351 mL 1.5878 mL
30 mM 0.0529 mL 0.2646 mL 0.5293 mL 1.3232 mL
40 mM 0.0397 mL 0.1985 mL 0.3969 mL 0.9924 mL
50 mM 0.0318 mL 0.1588 mL 0.3176 mL 0.7939 mL
60 mM 0.0265 mL 0.1323 mL 0.2646 mL 0.6616 mL
80 mM 0.0198 mL 0.0992 mL 0.1985 mL 0.4962 mL
100 mM 0.0159 mL 0.0794 mL 0.1588 mL 0.3969 mL
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Upamostat Related Classifications

Help & FAQs
  • 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.

Keywords:

Upamostat590368-25-5WX-671WX671WX 671PAI-1Ser/Thr ProteasePlasminogen activator inhibitor-1Serine proteasesSerine endopeptidasesThreonine proteasesuPA inhibitoramidoxime prodrugmARC enzyme systempharmacokineticspancreatic cancergemcitabine combination therapyInhibitorinhibitorinhibit

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Nombre del producto:
Upamostat
Cat. No.:
HY-16511
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