182705 | AhR Antagonist - CAS 301326-22-7 - Calbiochem

182705
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      Overview

      Key Spec Table

      Empirical FormulaCAS #
      C₁₉H₁₉N₅O301326-22-7

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      182705-10MG
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          10 mg
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          Description
          Overview A cell-permeable pyrazolo-amide compound that potently blocks the binding of TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) to AhR (aryl hydrocarbon receptor) in a dose-dependent manner. Shown to Inhibit TCDD-induced AhR transcription activity in HepG2 cells in vitro (IC50 = 30 nM) and prevent TCDD-elicited liver toxicity and wasting syndrome in mice in vivo. Unlike the commonly used AhR antagonist flavone, this inhibitor has no effect on estrogen receptor transcription activity, nor does it exhibit TCDD-like agonist activity even at concentrations as high as 10 µM.
          Catalogue Number 182705
          Brand Family Calbiochem®
          Synonyms 2-Methyl-2H-pyrazole-3-carboxylic acid-(2-methyl-4-o-tolyl-azophenyl)-amide, CH-223191
          References
          References Kim, S.H., et al. 2006. Mol. Pharmacol. 69, 1871.
          Product Information
          CAS number 301326-22-7
          ATP Competitive N
          Form Orange-brown
          Hill Formula C₁₉H₁₉N₅O
          Chemical formula C₁₉H₁₉N₅O
          Molar Mass 333.4
          Reversible N
          Structure formula Image
          Applications
          Biological Information
          Primary Target AhR (aryl hydrocarbon receptor)
          Primary Target IC<sub>50</sub> 30 nM in blocking TCDD-induced AhR transcription activity in HepG2 cells in vitro
          Purity ≥95% by HPLC
          Physicochemical Information
          Cell permeable Y
          Solubility DMSO
          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 Irritant
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze No
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          MSDS

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          Certificates of Analysis

          TitleLot Number
          182705

          References

          Reference overview
          Kim, S.H., et al. 2006. Mol. Pharmacol. 69, 1871.
          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.

          Revision 05-April-2011 RFH
          Synonyms 2-Methyl-2H-pyrazole-3-carboxylic acid-(2-methyl-4-o-tolyl-azophenyl)-amide, CH-223191
          Description A cell-permeable pyrazolo-amide compound that potently blocks the binding of TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) to AhR (aryl hydrocarbon receptor) in a dose-dependent manner. Shown to Inhibit TCDD-induced AhR transcription activity in HepG2 cells in vitro (IC50 = 30 nM) and prevent TCDD-elicited liver toxicity and wasting syndrome in mice in vivo. Unlike the commonly used AhR antagonist flavone, this inhibitor has no effect on estrogen receptor transcription activity, nor does it exhibit TCDD-like agonist activity even at concentrations as high as 10 µM.
          Form Orange-brown
          Intert gas (Yes/No) Packaged under inert gas
          CAS number 301326-22-7
          Molar mass 333.4
          Chemical formula C₁₉H₁₉N₅O
          Structure formula
          Purity ≥95% by HPLC
          Solubility DMSO (10 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          No
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Irritant
          References Kim, S.H., et al. 2006. Mol. Pharmacol. 69, 1871.