300266 | DP2 Antagonist II - Calbiochem

300266
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      Overview

      Replacement Information

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      300266-2MG
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          Glass bottle 2 mg
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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®
          SynonymsCRTH2 Antagonist II, GPR44 Antagonist II, (R)-(5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro(indole-3,3→-pyrrolidin)-1(2H)-yl)acetic acid
          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
          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

          References

          Reference overview
          Crosignani, S., et al. 2008. J Med Chem. 51, 2227.
          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.

          Revision12-April-2013 JSW
          SynonymsCRTH2 Antagonist II, GPR44 Antagonist II, (R)-(5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro(indole-3,3→-pyrrolidin)-1(2H)-yl)acetic acid
          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.