505765 Prostaglandin EP2 Receptor Antagonist, TG6-10-1 - Calbiochem

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

Synonyms: (E)-N-(2-(2-(trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide, EP2 Antagonist, TG6-10-1

Primary Target: EP2
505765
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₂₃F₃N₂O₄

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      5.05765.0001
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          		 Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, 3-acryl-acrylamide derivative that acts as a highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM). Exhibits about 300-fold selectivity for the EP2 receptor over human EP3, EP4, and IP receptors, about 100- fold selectivity over human EP1, 25-fold selectivity against human FP and TP, and 10-fold selectivity against human DP1 receptors. Does not affect the activity of about 40 enzymes, ion channels, receptors, and neurotransmitters even at higher concentrations (˜10 µM). Shown to significantly reduce the induction of several inflammatory cytokines and chemokines and reduces the opening of blood-brain barrier during neuronal inflammation. Displays good pharmacokinetic properties with a half-life of 1.6 h and brain to plasma ratio of 1.6 in a murine model (5 mg/kg i.p.).
          Catalogue Number505765
          Brand Family Calbiochem®
          Synonyms(E)-N-(2-(2-(trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide, EP2 Antagonist, TG6-10-1
          References
          ReferencesJ. Jiang et al. 2013, PNAS 110, 3591.
          Jiang. J et al. 2013, PNAS 109, 3149.
          Product Information
          FormWhite powder
          Hill FormulaC₂₃H₂₃F₃N₂O₄
          Chemical formulaC₂₃H₂₃F₃N₂O₄
          ReversibleY
          Structure formula ImageStructure formula Image
          Quality LevelMQ100
          Applications
          Biological Information
          Primary TargetEP2
          Primary Target K<sub>i</sub>17.8 nM
          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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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

          Prostaglandin EP2 Receptor Antagonist, TG6-10-1 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          J. Jiang et al. 2013, PNAS 110, 3591.
          Jiang. J et al. 2013, PNAS 109, 3149.
          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.

          Revision23-December-2013 JSW
          Synonyms(E)-N-(2-(2-(trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide, EP2 Antagonist, TG6-10-1
          DescriptionA cell-permeable, 3-acryl-acrylamide derivative that acts as a highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM). Exhibits about 300-fold selectivity for the EP2 receptor over human EP3, EP4, and IP receptors, about 100- fold selectivity over human EP1, 25-fold selectivity against human FP and TP, and 10-fold selectivity against human DP1 receptors. Does not affect the activity of about 40 enzymes, ion channels, receptors, and neurotransmitters even at higher concentrations (˜10 µM). Shown to significantly reduce the induction of several inflammatory cytokines and chemokines and reduces the opening of blood-brain barrier during neuronal inflammation. Displays good pharmacokinetic properties with a half-life of 1.6 h and brain to plasma ratio of 1.6 in a murine model (5 mg/kg i.p.).
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₃H₂₃F₃N₂O₄
          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 (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesJ. Jiang et al. 2013, PNAS 110, 3591.
          Jiang. J et al. 2013, PNAS 109, 3149.