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pKal-IN-1

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Catalog No. T218344 Copy Product Info
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pKal-IN-1 (compound 13) is an inhibitor of plasma kallikrein (pKal). It is applicable in research related to diabetic macular edema and diabetic retinopathy.

pKal-IN-1

Cas No. 2773609-90-6
Pack SizePriceUSA StockGlobal StockQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
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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Product Introduction

Bioactivity
Description
pKal-IN-1 (compound 13) is an inhibitor of plasma kallikrein (pKal). It is applicable in research related to diabetic macular edema and diabetic retinopathy.
In vitro
pKal-IN-1 (compound 13) is a potent inhibitor of plasma kallikrein with an IC50 of 0.7 nM. It does not exhibit time-dependent inhibition on CYP3A4, with a TDI ratio around 1. pKal-IN-1 shows no significant inhibition of hERG, with an IC50 > 60 μM. It activates PXR with an EC50 of 7.9 μM, achieving a maximum effect of 109%. Additionally, pKal-IN-1 inhibits CYP2C9 with an IC50 of 13 μM, but has no notable inhibitory effects on CYP2D6 or CYP2C8.
Chemical Properties
Molecular Weight489.85
FormulaC20H20ClF4N5O3
Cas No.2773609-90-6
SmilesFC1=C2[C@]3(CN(C(=O)C4=C(N)N([C@H](C(F)(F)F)CC)N=C4)CCC3)OC(=O)NC2=CC=C1Cl
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 µL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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g
µL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Related Tags: pKal-IN-1 in vitro | pKal-IN-1 formula | pKal-IN-1 molecular weight