[CAS NO. 256477-09-5] UK-371804
PRODUCTS SPECIFICATIONS [256477-09-5]
DESCRIPTION [256477-09-5]
Overview
| MDL | MFCD30742965 |
|---|---|
| Molecular Weight | 385.83 |
| Molecular Formula | C14H16ClN5O4S |
| SMILES | CC(C(O)=O)(C)NS(=O)(C1=CC2=C(C=C1)C(Cl)=CN=C2NC(N)=N)=O |
Summary
UK-371804 is a urokinase-type plasminogen activator ( uPA ) inhibitor with a K i 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 (IC 50 =0.89 μM). UK-371804 has its excellent enzyme potency (K i =10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : 8.33 mg/mL ( 21.59 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent 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 |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 0.83 mg/mL (2.15 mM); Clear solution