TAK-242

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TAK-242

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Cat No: 13871

Biochemicals - Receptor Pharmacology

TAK-242 is an antagonist of toll-like receptor 4 (TLR4) with an IC50 value of 0.68 µM in a secreted alkaline phosphatase (SEAP) assay.{60760} It selectively binds to TLR4 over TLR1-3 and TLR5-10 when used at a concentration of 100 nM.{28193} TAK-242 (...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

TAK242 TLR-1 2 4 5 6 7 8 9 TLR3 TLR10 HEK-293 IFN? TNF? IL6 IL1?

Product Overview:
TAK-242 is an antagonist of toll-like receptor 4 (TLR4) with an IC50 value of 0.68 µM in a secreted alkaline phosphatase (SEAP) assay.{60760} It selectively binds to TLR4 over TLR1-3 and TLR5-10 when used at a concentration of 100 nM.{28193} TAK-242 (1 µM) prevents the interaction of TLR4 with its adaptor proteins TIRAP or TRAM in HEK293 cells expressing the human receptors.{28193} It inhibits IFN-γ- and LPS-induced production of nitric oxide (NO), TNF-α, IL-6, and IL-1β in isolated mouse peritoneal macrophages (IC50s = 5.7-11 nM), as well as inhibits LPS-induced NETosis in isolated human neutrophils when used at concentrations ranging from 5 to 20 µM.{28174,60761} TAK-242 (0.3, 1, and 3 mg/kg) improves survival in a mouse model of septic shock induced by LPS.{28192}

Size	1 mg
Shipping	dry ice
CAS Number	243984-11-4
Molecular Formula	C₁₅H₁₇NO₄ClFS
SMILES	FC1=CC(Cl)=C(NS([C@@H]2CCCC=C2C(OCC)=O)(=O)=O)C=C1
Molecular Weight	361,8
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2935.90
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.