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TAK-242

Chemical Structure : TAK-242

CAS No.: 243984-11-4

TAK-242 (Resatorvid;TAK242;TAK 242;CLI-095)

Catalog No.: PC-42816Not For Human Use, Lab Use Only.

TAK-242 (Resatorvid) is a small molecule TLR4 signaling inhibitor that suppresses LPS-induced production of NO, TNF-alpha and IL-6 in RAW264.7 cells and mouse peritoneal macrophages with IC50 of 1.1-11 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TAK-242 (Resatorvid) is a small molecule TLR4 signaling inhibitor that suppresses LPS-induced production of NO, TNF-alpha and IL-6 in RAW264.7 cells and mouse peritoneal macrophages with IC50 of 1.1-11 nM.
TAK-242 also suppresses the production of these cytokines from LPS-stimulated human PBMCs with IC50 of 11-33 nM, suppresses the cytokine production induced by TLR-4 ligands, but not by ligands for TLR2, -3, and -9.
TAK-242 binds to Cys747 in the intracellular domain of TLR4, inhibits MyD88-independent pathway as well as MyD88-dependent pathway.
TAK-242 demonstrates potent therapeutic effects on mouse sepsis model.

Physicochemical Properties

M.Wt 361.8162
Formula C15H17ClFNO4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 360 mg/mL

Chemical Name/SMILES

1-Cyclohexene-1-carboxylic acid, 6-[[(2-chloro-4-fluorophenyl)amino]sulfonyl]-, ethyl ester, (6R)-

References

1. Yamada M, et al. J Med Chem. 2005 Nov 17;48(23):7457-67.

2. Ii M, et al. Mol Pharmacol. 2006 Apr;69(4):1288-95.

3. Sha T, et al. Eur J Pharmacol. 2007 Oct 1;571(2-3):231-9.

4. Takashima K, et al. Br J Pharmacol. 2009 Aug;157(7):1250-62.

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