532583 TLR1/TLR2 Agonist II, CU-T12-9 - Calbiochem

532583
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₃F₃N₄O₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.32583.0001
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          Glass bottle 10 mg
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          Description
          OverviewA diphenyl substituted imidazole based compound that directly and selectively targets TLR1/2 and induces their dimerization and activates TLR1 & 2 signaling leading to NF-κB and AP-1 activation (KD = 182 and 478 nM, respectively; EC50 = 52.9 nM for TLR2 in HEK-Blue cells over-expressing hTLR2). Does not affect the dimerization of TLR2/TLR6 and exhibits poor affinity towards TLR3, TLR4, TLR5, TLR7 and TLR8. Shown to compete with Pam3CSK4 (Cat. No. 506350; Ki = 45.4 nM) for binding to TLR1/2 interface and enhance heterodimerization. Up-regulates the expression of TLR1, TLR2, TNFα, IL-10, and iNOS in RAW 264.7 macrophages in a time-dependent manner. Shown to be non-toxic up to 100 µM concentration.

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number532583
          Brand Family Calbiochem®
          SynonymsN-Methyl-4-nitro-2-(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-1-yl)aniline, CUT129
          References
          ReferencesCheng, K., et al. 2014. Manuscript in preparation.
          Product Information
          FormYellow powder
          Hill FormulaC₁₇H₁₃F₃N₄O₂
          Chemical formulaC₁₇H₁₃F₃N₄O₂
          ReversibleY
          Applications
          Biological Information
          Primary TargetTLR1/TLR2
          Purity≥98% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          TLR1/TLR2 Agonist II, CU-T12-9 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Cheng, K., et al. 2014. Manuscript in preparation.
          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.

          Revision19-December-2014 JSW
          SynonymsN-Methyl-4-nitro-2-(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-1-yl)aniline, CUT129
          DescriptionA non-cytotoxic (up to 100 µM) diphenyl-substituted imidazole compound that exhibits high affinity toward both TLR1 & TLR2 (KD = 182 nM & 478 nM, respectively) and induces TLR1/2 heterodimerization, effectively completing against Pam3CSK4 (Cat. No. 506350) for TLR1/2 binding (Ki = 45.4 nM; [Pam3] = 20 mg/mL; [TLR1/2] = 80 nM). Shown to potently induce secreted embryonic alkaline phosphatase (SEAP) production from human TLR2-, but not TLR3-, 4-, 5-, 7-, 8-, transfected HEK293 (EC50 = 52.9 nM) in an NF-κB inhibitor Triptolide-(Cat. No. 645900) blockable manner via selective TLR1/2, but not TLR2/6, heterodimer activation. Reported to induce comparable NF-κB-dependent reporter transcription as 100 ng/mL Pam3CSK4 when administered to human macrophage U937 cultures at 5 µM concentration (24 h) and effectively trigger NO production in both murine Raw 264.7 and primary rat macrophage cultures (ECmax = 1.2 & 0.4 µM, respectively; 24 h), blockable by TLR1/2 antagonist CU-CPT22 (Cat. No. 614305), but not TLR4 antagonist TAK-242 (Cat. No. 614316 & 508336). Likewise, both CU-T12-9 and Pam3CSK4 (1 µM & 50 ng/mL, respectively) are demonstrated to induce similar time-dependent induction of TLR1, TLR2, TNF-α, iNOS, IL-10 mRNA in Raw 264.7 cells.
          FormYellow powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₇H₁₃F₃N₄O₂
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesCheng, K., et al. 2014. Manuscript in preparation.