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614316 TLR4 Inhibitor, TAK-242 - CAS 243984-11-4 - Calbiochem

TAK-242; CAS 243984-11-4; is a cell-permeable compound that selectively binds to Cys747 of TLR4 and selectively disrupts its interaction with adaptor molecules TIRAP and TRAM.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Ethyl-(6R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate

Primary Target: TLR4
614316
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Overview

Key Spec Table

CAS #Empirical Formula
243984-11-4C₁₅H₁₇ClFNO₄S

Products

Catalogue NumberPackaging Qty/Pack
614316-5MG Glass bottle 5 mg
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Description
OverviewA cell-permeable cyclohexenecarboxylate that disrupts TLR4, but not TLR1-3 or TLR5-10, interaction with adaptor molecules TIRAP and TRAM via direct binding to TLR4 intracellular Cys747 residue.Shown to effectively inhibit TLR4-mediated cellular events (IC50 = 1.8, 1.3, and 1.9 nM, respectively, against LPS-induced NO, IL-6, and TNF-α production in murine RAW264.7 macrophages) in vitro and completely prevent LPS- (7 mg/kg, i.p.) induced death in mice (3 mg/kg; i.v.) in vivo. Also available as a 25 mM solution in DMSO (Cat. No. 508336).
Catalogue Number614316
Brand Family Calbiochem®
SynonymsEthyl-(6R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate
References
ReferencesMatsunaga, N., et al. 2011. Mol. Pharmacol. 79, 34.
Takashima, K., et al. 2009. Br. J. Pharmacol. 157, 1250.
Li, M., et al. 2006. Mol. Pharmacol. 69, 1288.
Yamada, M., et al. 2005. J. Med. Chem. 48, 7457.
Product Information
CAS number243984-11-4
FormWhite to yellowish white solid
Hill FormulaC₁₅H₁₇ClFNO₄S
Chemical formulaC₁₅H₁₇ClFNO₄S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Primary TargetTLR4
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Safety Information
R PhraseR: 22

Harmful if swallowed.
S PhraseS: 26-36

In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
Wear suitable protective clothing.
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Harmful
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 1 year at -70°C. Use only fresh DMSO.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
614316-5MG 04055977186635