UK-371804 is a potent and selective uPA inhibitor with excellent enzyme potency (Ki 10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). In vitro, UK-371804 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 microM). 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. UK-371804 was selected as a candidate for further preclinical evaluation for the treatment of chronic dermal ulcers.
MedKoo Cat#: 206487
Name: UK-371804
CAS#: 256477-09-5 (free base)
Chemical Formula: C14H16ClN5O4S
Exact Mass: 385.0612
Molecular Weight: 385.82
Elemental Analysis: C, 43.58; H, 4.18; Cl, 9.19; N, 18.15; O, 16.59; S, 8.31
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.0 | 2.59 |
The following data is based on the product molecular weight 385.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
