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300266 DP2 Antagonist II - Calbiochem

300266
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300266-2MG
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      Description
      OverviewThe (R) enantiomer of a cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 5.3 and 5.0 nM against human & murine DP2, respectively), exhibiting much reduced potency against a panel of more than 50 other receptors and ion channels. Effectively inhibits DP2-dependent chemotaxis of primary human eosinophils (IC50 = 100 nM). Exhibits higher Caco-2 permeability than DP2 Antagonist I (Cat. No. 300264), but less oral bioavailability in mice.
      Catalogue Number300266
      Brand Family Calbiochem®
      Synonyms(R)-(5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro(indole-3,3→-pyrrolidin)-1(2H)-yl)acetic acid, CRTH2 Antagonist II, GPR44 Antagonist II
      References
      ReferencesCrosignani, S., et al. 2008. J Med Chem. 51, 2227.
      Product Information
      FormWhite powder
      Hill FormulaC₂₀H₁₃Cl₂FN₂O₅
      Chemical formulaC₂₀H₁₃Cl₂FN₂O₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetDP2
      Primary Target K<sub>i</sub>5.3 nM
      Purity≥93% 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 Yes
      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

      Références bibliographiques

      Aperçu de la référence bibliographique
      Crosignani, S., et al. 2008. J Med Chem. 51, 2227.
      Fiche technique

      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.

      Revision12-April-2013 JSW
      Synonyms(R)-(5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro(indole-3,3→-pyrrolidin)-1(2H)-yl)acetic acid, CRTH2 Antagonist II, GPR44 Antagonist II
      DescriptionThe (R) enantiomer of a cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 5.3 and 5.0 nM against 1.5 nM PGD2 for human & murine DP2 binding, respectively), exhibiting much reduced or little potency against a panel of more than 50 other receptors and ion channels, including PGD2 receptor DP1, PGE receptors (EP2, EP3, EP4), and PGF receptor FP (IC50 >30 µM). Effectively inhibits DP2-dependent chemotaxis of primary human eosinophils (IC50 = 100 nM; chemotractant = 100 nM DK-PGD2) in vitro. Shown to exhibit higher Caco-2 permeability than DP2 Antagonist I (Cat. No. 300264; Papp in unit of 10-6 cm/s = 26.4 vs. 5.2, respectively), but less oral bioavailability (32% in rat for Inhibitor II vs. 80% in mice for Inhibitor I with same oral dosage of 5 mg/kg).
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₀H₁₃Cl₂FN₂O₅
      Structure formulaStructure formula
      Purity≥93% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Yes
      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. 2008. J Med Chem. 51, 2227.