| CAS NO: | 256476-36-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 422.29 |
|---|---|
| Formula | C14H16ClN5O4S.HCl |
| CAS No. | 256476-36-5; |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 42 mg/mL (99.5 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES Code | CC(C)(NS(=O)(C1=CC2=C(C=C1)C(Cl)=CN=C2/N=C(N)\N)=O)C(O)=O.[H]Cl |
| Synonyms | UK371804; UK-371804; UK 371804; UK-371,804; UK 371,804; UK371,804. |
| In Vitro | In vitro activity: UK-371804 is a potent and selective inhibitor of urokinase-type plasmogen activator (uPA) with excellent potency (Ki=10 nM in an enzyme assay) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). UK-371804 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 microM) in vitro. In a porcine acute excisional wound model in vivo, upon topical administration, UK-371804 is able to penetrate into pig wounds and inhibit exogenous uPA activity with no adverse side effects on wound healing parameters. Kinase Assay: 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. Cell Assay: |
|---|---|
| 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 |
| Animal model | Pig |
| Formulation & Dosage | 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. |
| References | J Med Chem. 2007 May 17;50(10):2341-51. |
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