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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
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Overview

Key Spec Table

CAS #Empirical Formula
243984-11-4C₁₅H₁₇ClFNO₄S

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614316-5MG
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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