TAK 242

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Description: TLR4 signaling inhibitor
Chemical Name: (R)-Ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Reviews
Pathways (1)

Biological Activity for TAK 242

TAK 242 is a toll-like receptor 4 (TLR4) signaling inhibitor. Binds to intracellular domain of TLR4. Inhibits LPS-induced cytokine production in vitro (IC50 values are 1.3, 1.3 and 3.2 nM for IL-6, TNFα and NO production). Reduces lesion volume in a mouse model of cerebral cavernous malformations (CCMs). Also attenuates increased cytokine levels in a mouse sepsis model, when given in combination with ceftazidime. Cell permeable.

Technical Data for TAK 242

M. Wt 361.82
Formula C15H17ClFNO4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 243984-11-4
PubChem ID 11703255
InChI Key LEEIJTHMHDMWLJ-CQSZACIVSA-N
Smiles CCOC(C1=CCCC[C@H]1S(=O)(NC2=C(C=C(C=C2)F)Cl)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for TAK 242

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.18 100
ethanol 36.18 100

Preparing Stock Solutions for TAK 242

The following data is based on the product molecular weight 361.82. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.76 mL 13.82 mL 27.64 mL
5 mM 0.55 mL 2.76 mL 5.53 mL
10 mM 0.28 mL 1.38 mL 2.76 mL
50 mM 0.06 mL 0.28 mL 0.55 mL

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Product Datasheets for TAK 242

Certificate of Analysis / Product Datasheet
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Keywords: TAK 242, TAK 242 supplier, TAK242, toll, like, receptor, TLR4, signaling, inhibitor, inhibits, sepsis, cell, permeable, Toll-like, Receptors, 6587, Tocris Bioscience

6 Citations for TAK 242

Citations are publications that use Tocris products. Selected citations for TAK 242 include:

Titus Ikusya et al (2022) Bodyweight, locomotion, and behavioral responses of the naked mole rat (Heterocephalus glaber) to lipopolysaccharide administration. J Comp Physiol A Neuroethol Sens Neural Behav Phys 208 493-504 PMID: 35731263

Harpal S et al (2022) Asprosin Exerts Pro-Inflammatory Effects in THP-1 Macrophages Mediated via the Toll-like Receptor 4 (TLR4) Pathway. Int J Mol Sci 24 PMID: 36613673

Emre et al (2022) Opioid Antagonist Nanodrugs Successfully Attenuate the Severity of Ischemic Stroke. Mol Pharm 19 2254-2267 PMID: 35506882

Robert A et al (2022) Human platelets display dysregulated sepsis-associated autophagy, induced by altered LC3 protein-protein interaction of the Vici-protein EPG5. Autophagy 18 1534-1550 PMID: 34689707


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Pathways for TAK 242

Toll-like Receptor Signaling Pathway

Toll-like Receptor Signaling Pathway

TLR signaling is involved in the cellular response to threatening molecules such as bacteria and viruses. It results in an inflammatory and immmunological response.