Home Proteases Serine Protease inhibitor UK-371804 HCl

UK-371804 HCl

Catalog No.S8457

For research use only.

UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

UK-371804 HCl Chemical Structure

CAS No. 256476-36-5

Selleck's UK-371804 HCl has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).
Targets
uPA [1]
(Cell-free assay)
10 nM(Ki)
In vitro

In Vitro, UK-3718046 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 µM)[1].
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[1].

Protocol (from reference)

Animal Research:[1]
  • Animal Models: A porcine acute excisional wound model
  • Dosages: 10 mg/mL
  • Administration: topical delivery

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 422.29
Formula

C14H16ClN5O4S.HCl
CAS No. 256476-36-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C(=O)O)NS(=O)(=O)C1=CC2=C(C=C1)C(=CN=C2N=C(N)N)Cl.Cl

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04705766 Recruiting Other: Urine Collection SARS-CoV Infection|Covid19|Corona Virus Infection|Acute Kidney Injury|Kidney Injury University of California San Francisco|Rush University Medical Center|University of Michigan|University of California|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) March 1 2021 --
NCT04588220 Active not recruiting Other: Obstetric ultrasound and fetal-maternal assessment Preterm Premature Rupture of Membranes Cengiz Gokcek Women''s and Children''s Hospital October 7 2020 --
NCT04688879 Completed Procedure: intra-arterial urokinase thrombolysis Arterial Occlusion Mesenteric Artery Superior Chang Gung Memorial Hospital March 1 2020 --
NCT03769337 Unknown status Diagnostic Test: serum biomarkers Prosthetic Joint Infections Istituto Ortopedico Galeazzi September 1 2018 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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