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UK-371804 Urokinase inhitibor 1 256477-09-5
UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
| Cas No. | 256477-09-5 |
Canonical SMILES | CC(C(O)=O)(C)NS(=O)(C1=CC2=C(C=C1)C(Cl)=CN=C2NC(N)=N)=O |
Formula | C14H16ClN5O4S |
M.Wt | 385.83 |
Storage | Store at -20°C |
Solubility | DMSO : 10 mg/mL (25.92 mM) |
General tips | Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. |
| To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
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 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:
[1]. Fish PV, et al. Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. J Med Chem. 2007 May 17;50(10):2341-51.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.