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300264 DP2 Antagonist I - Calbiochem

300264
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300264-2MG
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      Glass bottle 2 mg
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      Description
      OverviewA cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 2.0 and 2.4 nM against 1.5 nM PGD2 for human & murine DP2 binding, respectively), exhibiting much reduced potency against DP1 (Ki = 1.58 µM; IC50 = 10 µM), PGE receptor EP2 (54% inhibition at 10 µM), and little or no activity toward 49 other receptors and ion channels. Effectively inhibits PGD2-induced cellular activation (IC50 = 32 and 80 nM, respectively, using CHO-CRTH2 or human whole blood) in vitro and is efficacious in alleviating airway eosinophil infiltration in OVA- (Cat. No. 32467) sensitized mice (30 mg/kg; p.o.) in vivo with good oral bioavailability.
      Catalogue Number300264
      Brand Family Calbiochem®
      Synonyms(4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid, CRTH2 Antagonist I, GPR44 Antagonist I
      References
      ReferencesCrosignani, S., et al. 2011. J Med Chem. 54, 7299.
      Product Information
      FormWhite powder
      Hill FormulaC₂₀H₁₉ClO₅S
      Chemical formulaC₂₀H₁₉ClO₅S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetDP2
      Primary Target K<sub>i</sub>2 nM
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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

      References

      Reference overview
      Crosignani, S., et al. 2011. J Med Chem. 54, 7299.
      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-March-2013 JSW
      Synonyms(4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid, CRTH2 Antagonist I, GPR44 Antagonist I
      DescriptionA cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 2.0 and 2.4 nM against 1.5 nM PGD2 for human & murine DP2 binding, respectively), inhibiting AR (aldose reductase) only at higher concentrations (IC50 = 172 nM) and exhibiting much reduced potency against PGD2 receptor DP1 (Ki = 1.58 µM; IC50 = 10 µM), PGE receptor EP2 (54% binding inhibition at 10 µM), and little or no activity toward 49 other receptors and ion channels (IC50 >10 µM). Effectively inhibits PGD2-induced cellular activation (IC50 = 32 and 80 nM, respectively, using CHO-CRTH2 or human whole blood) in vitro and is efficacious in alleviating airway eosinophil infiltration in OVA- (Cat. No. 32467) sensitized mice (3.1- and 5.8-fold of control, respectively, with or without 30 mg/kg oral dosages 1 h before and 7 h after each of three daily 30-min OVA aerosol challenges) in vivo with good oral bioavailability (t1/2 = 3.9; AUC = 3730 ng·h/mL; 5 mg/kg p.o.).
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₀H₁₉ClO₅S
      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
      ReferencesCrosignani, S., et al. 2011. J Med Chem. 54, 7299.