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ZK824859 Serine Protease inhibitor

Name: ZK824859
Brand: Selleck Chemicals
SKU: S0479
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S0479

ZK824859 is a potent, selective and orally bioavailable inhibitor of urokinase plasminogen activator (uPA) with IC50 of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.

Chemical Structure

Molecular Weight: 414.40

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S047901 DMSO]86 mg/mL]false]Ethanol]86 mg/mL]false]Water]Insoluble]false Purity: 99.86%

99.86

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Chemical Information, Storage & Stability

Molecular Weight	414.40	Formula	C₂₂H₂₀F₂N₂O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2254001-81-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCC(C(=O)O)OC1=C(C=C(C(=N1)OC2=CC(=CC(=C2)C3=CC=CC(=C3)CN)C)F)F

Solubility

In vitro
Batch:

DMSO : 86 mg/mL ( (207.52 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
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.	3.250mg/ml (7.84mM)	Taking the 1 mL working solution as an example, add 50 μL of 65 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.	0.540mg/ml (1.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.8 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.

Mechanism of Action

Targets/IC₅₀/Ki	human uPA ^[1] (Cell-free assay) 79 nM human plasmin ^[1] (Cell-free assay) 1330 nM human tPA ^[1] (Cell-free assay) 1580 nM
In vivo	ZK824859, a selective and orally bioavailable inhibitor of uPA, lowers clinical scores when dosed in both acute and chronic mouse EAE models.^[1]
References	https://pubmed.ncbi.nlm.nih.gov/30201291/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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