In vitro: UK-3718046 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 µM). In vivo: In Vivo, in a porcine acute excisional wound model, following topical delivery, UK-3718046 is able to penetrate into pig wounds and inhibit exogenous uPA activity with no adverse effect on wound healing parameters.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | A porcine acute excisional wound model |
| Formulation | hydrogel vehicle |
| Dosages | 10 mg/mL |
| Administration | 10 mg/mL |
| Molecular Weight | 383.75 |
| Formula | C14H16ClN5O4S |
| CAS Number | 256477-09-5 |
| Solubility (25°C) | 42 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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