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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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|
References are publications that support the biological activity of the product.
Yamada et al (2005) 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. 48 7457 PMID: 16279805
Ii et al (2006) 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. 69 1288 PMID: 16373689
Tang et al (2017) Endothelial TLR4 and the microbiome drive cerebral cavernous malformations. Nature 545 305 PMID: 28489816
Takashima et al (2009) 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. 157 1250 PMID: 19563534
If you know of a relevant reference for TAK 242, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: TAK 242, TAK 242 supplier, TAK242, toll, like, receptor, TLR4, signaling, inhibitor, inhibits, sepsis, cell, permeable, Toll-like, Receptors, 6587, Tocris Bioscience
Citations for TAK 242
Citations are publications that use Tocris products.
Currently there are no citations for TAK 242. Do you know of a great paper that uses TAK 242 from Tocris? Please let us know.
Reviews for TAK 242
There are currently no reviews for this product. Be the first to review TAK 242 and earn rewards!
Have you used TAK 242?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.