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

UK-371804 

Cat. No.: HY-101214 Purity: >98.0%
Data Sheet SDS Handling Instructions

UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.

For research use only. We do not sell to patients.
UK-371804 Chemical Structure

UK-371804 Chemical Structure

CAS No. : 256477-09-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO $132 In-stock
5 mg $120 In-stock
10 mg $210 In-stock
50 mg $650 In-stock
100 mg $950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.

IC50 & Target

Ki: 10 nM (uPA)[1]

In Vitro

UK-371804 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 μM). UK-371804 has its excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin)[1].

In Vivo

In a porcine acute excisional wound model, following topical delivery, UK-371804 is able to penetrate into pig wounds and inhibit exogenous uPA activity with no adverse effect on wound healing parameters. Concentrations of UK-371804 in the dermis are 41.8 μM[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.5918 mL 12.9591 mL 25.9182 mL
5 mM 0.5184 mL 2.5918 mL 5.1836 mL
10 mM 0.2592 mL 1.2959 mL 2.5918 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

UK-371804 is formulated in hydrogel.

Pig: Two female pigs are subjected to eight excisional wounds. The wounds are dressed and treated daily for 10 days with either 1 mL of a 10 mg/mL formulation of UK-371804 in hydrogel vehicle, or hydrogel vehicle alone (control). On day 11 the animals are sacrificed, terminal blood samples are taken to assess any systemic exposure of the compounds, and the wounds are excised from the surrounding normal skin[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

385.83

Formula

C₁₄H₁₆ClN₅O₄S

CAS No.

256477-09-5

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

Solvent & Solubility

DMSO: 10 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
UK-371804
Cat. No.:
HY-101214
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