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

614316
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₁₇ClFNO₄S 243984-11-4

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      614316-5MG
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          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
          Applications
          Biological Information
          Primary TargetTLR4
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          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.
          Product Usage Statements
          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
          Transport Information
          Supplemental Information
          Specifications

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          TLR4 Inhibitor, TAK-242 - CAS 243984-11-4 - Calbiochem Certificates of Analysis

          TitleLot Number
          614316

          References

          Reference overview
          Matsunaga, 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.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision27-February-2018 JSW
          SynonymsEthyl-(6R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate
          DescriptionA cell-permeable cyclohexenecarboxylate that disrupts TLR4 interaction with adaptor molecules TIRAP and TRAM by selectively binding to TLR4, but not TLR1-3 or TLR5-10, via TLR4 intracellular Cys747 residue. Shown to effectively inhibit TLR4-mediated signaling events, including LPS-induced NO and inflammatory cytokines production in murine RAW264.7 macrophages (IC50 = 1.8, 1.3, and 1.9 nM, respectively, against NO, IL-6, and TNF-α production), TLR4/TIRAP-dependent NF-κB activity as well as TLR4/TIRAP- and TLR4/TRAM-dependent ISRE activity (IC50 < 300 nM) in HEK293-hTLR4/MD2-CD14 transfected with either TIRAP or TRAM. When administered at an i.v. dose of 3 mg/kg, TAK-242 is reported to completely prevent LPS- (7 mg/kg, i.p.) induced death in mice in vivo. Complete elimination of septic shock-induced death can be extended to live E. coli-infected mice when co-administered with ceftazidime (3 mg/kg TAK-242 and 20 mg/kg ceftazidime, i.v.).
          FormWhite to yellowish white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number243984-11-4
          Chemical formulaC₁₅H₁₇ClFNO₄S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          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.
          Toxicity Harmful
          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.