TAK 242

Name: TAK 242
Brand: Tocris Bioscience
SKU: 6587

Tocris Bioscience, part of Bio-Techne | Catalog # 6587

Citations (29)

COA / SDS

TLR4 signaling inhibitor

Key Product Details

Description:	TLR4 signaling inhibitor
Chemical Name:	(R)-Ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate
Purity:	≥98% (HPLC)
Molecular Weight:	361.82

View Full Technical Details for TAK 242

Technical Data
Citations

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 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.

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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References for TAK 242

References are publications that support the biological activity of the product.

Takashima Analysis of binding site for the novel small-molecule TLR4 signal transduction inhibitor TAK-242 and its therapeutic effect on mouse sepsis model. Br.J.Pharmacol. 2009 PMID: 19563534
Ii A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signal Mol.Pharmacol. 2006 PMID: 16373689
Tang Endothelial TLR4 and the microbiome drive cerebral cavernous malformations. Nature 2017 PMID: 28489816
Yamada Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate. J.Med.Chem. 2005 PMID: 16279805