Home Cytoskeletal Signaling Integrin inhibitor A-205804

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A-205804 Integrin inhibitor

Cat.No.S2885

A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively.
A-205804 Integrin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 300.4

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Quality Control

Batch: S288501 DMSO]60 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.66%
99.66

Chemical Information, Storage & Stability

Molecular Weight 300.4 Formula

C15H12N2OS2

 Storage (From the date of receipt)
CAS No. 251992-66-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC=C(C=C1)SC2=C3C=C(SC3=CN=C2)C(=O)N

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (199.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.
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Mechanism of Action

Targets/IC50/Ki
E-selectin [1]
20 nM
ICAM-1 [1]
25 nM
In vitro
A-205804 selectively inhibits the surface expression of the cell adhesion molecules ICAM-1 and E-selectin in human endothelial cells. This compound inhibites the IL-1β-induced expression of E-selectin (IC50 = 20 nM) and ICAM-1 (IC50 = 10 nM) with essentially the same level of potency as that for TNFα-induced expression. For reasons which are unclear, the ability of this chemical to inhibit PMA-induced E-selectin expression is significantly reduced (IC50 > 1000 nM), but it is a potent inhibitor of ICAM-1 expression (IC50 = 40 nM) using this protein-kinase C-activating agent. [2]
References

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