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UK-371804 HCl Serine Protease inhibitor

Name: UK-371804 HCl
Brand: Selleck Chemicals
SKU: S8457
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8457

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).

Chemical Structure

Molecular Weight: 422.29

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Quality Control

Batch: Purity: 99.56%

99.56

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease
Other Serine Protease Inhibitors	Leupeptin Hemisulfate PMSF Nafamostat mesilate (FUT-175) Sivelestat AEBSF HCl Gabexate Mesylate Alvelestat (AZD9668) Sivelestat sodium tetrahydrate Ulinastatin Fulacimstat

Solubility

In vitro
Batch:

DMSO : 42 mg/mL (99.45 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.850mg/ml (2.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 17 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.850mg/ml (2.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 17 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	422.29	Formula	C₁₄H₁₆ClN₅O₄S.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	256476-36-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)(C(=O)O)NS(=O)(=O)C1=CC2=C(C=C1)C(=CN=C2N=C(N)N)Cl.Cl

Mechanism of Action

Targets/IC₅₀/Ki	uPA (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).
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17447747/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06349590	Not yet recruiting	Colorectal Cancer	University of Chicago	April 2024	Phase 1\|Phase 2
NCT05286710	Recruiting	Deep Vein Thrombosis	RenJi Hospital\|First People''s Hospital of Hangzhou\|The First Affiliated Hospital with Nanjing Medical University\|Affiliated Hospital of Nantong University\|Chengdu University of Traditional Chinese Medicine\|Second Affiliated Hospital of Suzhou University\|Liuzhou Workers Hospital\|Shanghai Pudong New Area People''s Hospital\|Zhejiang University	October 26 2022	Not Applicable
NCT05356767	Recruiting	Pharmacomechanical Thrombolysis\|Deep Vein Thrombosis	Chengdu University of Traditional Chinese Medicine	April 1 2022	--
NCT04705766	Recruiting	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	March 1 2021	--
NCT04796493	Active not recruiting	Mesenteric Traction Syndrome	Rigshospitalet Denmark	March 16 2021	--

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