TAK 242

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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