UK-371804

SKU: orb1225497

Description

UK-371804 is a potent and selective inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 10 nM; displays excellent selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin); inhibits exogenous uPA in human chronic wound fluid with IC50 of 0.89 uM; penetrates into pig wounds and inhibits exogenous uPA activity with no adverse effect on wound healing parameters in wound model following topical delivery.Ulcer Preclinical.

Key Properties

• CAS Number: 256477-09-5
• MW: 385.82594
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₆ClN₅O₄S
• SMILES: CC(C)(NS(=O)(C1=CC2=C(C=C1)C(Cl)=CN=C2/N=C(N)\N)=O)C(O)=O
• Target: PAI-1
• Solubility: DMSO: 10 mg/mL

Bioactivity

• 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.
• In Vitro:
  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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

UK371804 | UK 371804

Quick Database Links

Gene Symbol

PAI-1