Home Proteases Cysteine Protease inhibitor PD 151746

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PD 151746 Cysteine Protease inhibitor

Cat.No.S7424

PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.
PD 151746 Cysteine Protease inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 237.25

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

Quality Control

Batch: S742401 DMSO]47 mg/mL]false]Ethanol]47 mg/mL]false]Water]Insoluble]false Purity: 98.59%
98.59

Chemical Information, Storage & Stability

Molecular Weight 237.25 Formula
C11H8FNO2S
 
 Storage (From the date of receipt)
CAS No. 179461-52-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC2=C(C=C1F)C(=CN2)C=C(C(=O)O)S

Solubility

In vitro
Batch:

DMSO : 47 mg/mL (198.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
% Tween 80
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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
μ-Calpain [1]
260 nM
m-calpain [1]
5.33 μM
In vitro
In SY5Y cells, PD151746 effectively attenuates the SLLVY-AMC hydrolysis induced by maitotoxin. [1] In HMEC-1 cells, PD 151746 decreases cytotoxicity induced by oxidized low-density lipoprotein (oxLDL). [2]
References

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