[CAS NO. 243984-11-4] Resatorvid (TAK-242)

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PRODUCTS SPECIFICATIONS [243984-11-4]

Catalog

SLK-S7455

Brand

Selleck

CAS

243984-11-4

DESCRIPTION [243984-11-4]

Overview

MDL	MFCD11046362
Molecular Weight	361.82
Molecular Formula	C15H17ClFNO4S
SMILES	S(NC1=C(Cl)C=C(F)C=C1)(=O)(=O)[C@H]2C(C(OCC)=O)=CCCC2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.7638 mL	13.8190 mL	27.6381 mL
5 mM	0.5528 mL	2.7638 mL	5.5276 mL
10 mM	0.2764 mL	1.3819 mL	2.7638 mL
50 mM	0.0553 mL	0.2764 mL	0.5528 mL

Description

Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of , blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits .

Targets

TLR4 ^[1]	IL-6 ^[5] (Cell-free assay)	NO ^[5] (Cell-free assay)	TNF-α ^[5] (Cell-free assay)
	1.3 nM	1.8 nM	1.9 nM

In vitro

TAK-242 inhibits the TLR4 pathway by binding directly to a Cys747 in the intracellular TLR4 domain. TAK-242 disrupts the interactions of TLR4 with its adaptor molecules, TIRAP and TRAM.

References

[1] Kuzmich NN, et al. Vaccines (Basel). 2017, 5(4). pii: E34.
[2] Blohm-Mangone K, et al. Cancer Prev Res (Phila). 2018, 11(5):265-278.
[3] Suzuki Y, et al. Sci Rep. 2012, 2:896.
[4] Janda J, et al. Photochem Photobiol. 2016, 92(6):816-825.
[5] Masami Yamada, et al. J Med Chem . 2005 Nov 17;48(23):7457-67.

Synonyms

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

TAK 242

Resatorvid