ZK824190

Cat. No.: HY-126361: FAQs
Data Sheet Handling Instructions

Molarity Calculator

ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC₅₀s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (ZK824190 hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

ZK824190 Chemical Structure

CAS No. : 2254001-81-3

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50 mg		Get quote
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250 mg		Get quote
Other size		Get quote

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Other In-stock Forms of ZK824190:

Other Forms of ZK824190:

ZK824190 hydrochloride In-stock

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC50: 237 nM (uPA), 1600 nM (tPA), 1850 nM (Plasmin)^[1]

In Vivo

ZK824190 (2 mg/kg; PO) exhibits a relatively high oral availability and a moderate half time (T_1/2=2.8 h)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Rats with experimental autoimmune encephalomyelitis (EAE) model^[1]
Dosage:	2 mg/kg (Pharmacokinetic Analysis)
Administration:	PO
Result:	Oral availability F = 55%; C_max= 0.64 g/mL and AUC = 2.2 h*g/mL; T_1/2=2.8 h.

Molecular Weight

414.40

Formula

C₂₂H₂₀F₂N₂O₄

CAS No.

2254001-81-3

SMILES

CC[C@@H](OC1=NC(OC2=CC(C3=CC=CC(CN)=C3)=CC=C2)=C(F)C=C1F)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (603.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4131 mL	12.0656 mL	24.1313 mL
5 mM	0.4826 mL	2.4131 mL	4.8263 mL
10 mM	0.2413 mL	1.2066 mL	2.4131 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Islam I, et al. Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3372-3375. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4131 mL	12.0656 mL	24.1313 mL	60.3282 mL
	5 mM	0.4826 mL	2.4131 mL	4.8263 mL	12.0656 mL
	10 mM	0.2413 mL	1.2066 mL	2.4131 mL	6.0328 mL
	15 mM	0.1609 mL	0.8044 mL	1.6088 mL	4.0219 mL
	20 mM	0.1207 mL	0.6033 mL	1.2066 mL	3.0164 mL
	25 mM	0.0965 mL	0.4826 mL	0.9653 mL	2.4131 mL
	30 mM	0.0804 mL	0.4022 mL	0.8044 mL	2.0109 mL
	40 mM	0.0603 mL	0.3016 mL	0.6033 mL	1.5082 mL
	50 mM	0.0483 mL	0.2413 mL	0.4826 mL	1.2066 mL
	60 mM	0.0402 mL	0.2011 mL	0.4022 mL	1.0055 mL
	80 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7541 mL
	100 mM	0.0241 mL	0.1207 mL	0.2413 mL	0.6033 mL

ZK824190 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZK8241902254001-81-3ZK 824190ZK-824190Ser/Thr ProteasePAI-1Serine proteasesSerine endopeptidasesThreonine proteasesPlasminogen activator inhibitor-1uPAUrokinaseSerineproteaseplasminogenmultiple sclerosisInhibitorinhibitorinhibit

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