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Resatorvid (TAK-242) TLR4 inhibitor

Cat.No.S7455

Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. This compound downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF, and it also inhibits autophagy.
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Quality Control

Batch: Purity: 99.92%
99.92

Solubility in DMSO or Water

In vitro
Batch:

DMSO : 72 mg/mL (198.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 72 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

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Working Concentrations for Cell Culture Treatment

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Working Concentrations for Animal Model Treatment

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Mechanism of Action

Information Resatorvid (TAK-242) is a selective TLR4 inhibitor. It affects TLR4/MyD88/NF-κB and NLRP3 signaling by binding to the TLR4 intracellular domain, effectively inhibiting inflammatory cytokine production, apoptosis, and cell migration.
Primary Applications and Mechanism of Action

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Chemical Information, Storage & Stability

Molecular Weight 361.82 Formula

C15H17ClFNO4S

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 243984-11-4 -- Storage of Stock Solutions

Synonyms CLI-095 Smiles CCOC(=O)C1=CCCCC1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl

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