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PKSI-527

Name: PKSI-527
Brand: TargetMol
SKU: T35579
Rating: 4.5 (1 reviews)

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Catalog No. T35579 Copy Product Info

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PKSI-527 is a non-covalent, highly selective small molecule inhibitor of plasma kallikrein with an inhibition constant (Ki) of 0.81 µM for plasma kallikrein. PKSI-527 modulates the kallikrein-kinin system by inhibiting bradykinin generation, significantly reduces arthritis severity in a collagen-induced arthritis mouse model, and improves indicators of disseminated intravascular coagulation and organ damage in endotoxin-induced rat models.

Cas No. 128837-71-8

Pack Size	Price	USA Stock	Global Stock	Quantity
2 mg	$78	5 days	5 days

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Appearance:Viscous

Color:Transparent

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Product Introduction

Bioactivity

Description

In vivo

In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.

Chemical Properties

Molecular Weight	473.99
Formula	C₂₅H₃₂ClN₃O₄
Cas No.	128837-71-8
Smiles	[C@@H](CC1=CC=CC=C1)(NC(=O)[C@H]2CC[C@H](CN)CC2)C(NC3=CC=C(CC(O)=O)C=C3)=O.Cl
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (168.78 mM), Sonication is recommended.

H2O: 10 mM, Sonication is recommended.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1097 mL	10.5487 mL	21.0975 mL	105.4875 mL
5 mM	0.4219 mL	2.1097 mL	4.2195 mL	21.0975 mL
10 mM	0.2110 mL	1.0549 mL	2.1097 mL	10.5487 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.1055 mL	0.5274 mL	1.0549 mL	5.2744 mL
50 mM	0.0422 mL	0.2110 mL	0.4219 mL	2.1097 mL
100 mM	0.0211 mL	0.1055 mL	0.2110 mL	1.0549 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.