300264 | DP2 Antagonist I - Calbiochem

300264
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      300264-2MG
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service

          Glass bottle 2 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          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
          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.