317701 Dkk Inhibitor II, IIIC3a - Calbiochem

317701
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      317701-25MG
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          25 mg
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          Description
          OverviewAn enhanced in solution stable gallocyanine analog that directly and reversibly targets human LRP5/6 (low density lipoprotein-related protein 5/6), and disrupts its interaction with Dkk (Dickkopf) in a competitive manner. Shown to potently reverse DKK1/2/4-mediated inhibition of WNT3A-stimulated reporter gene activity (IC50 ~ 10 - 30 µM in in NIH 3T3 cells) with no effects on sFRP4-mediated inhibition of Wnt signaling. Blocks Dkk-2 - alkaline phosphatase binding to cells expressing LRP5 (IC50 = 1 µM in LRP5 transfected NIH 3T3 cells). Reduces blood glucose levels, improves glucose tolerance, and increases insulin sensitivity in type 2 diabetic mice (1.5 mg/kg, i.p. daily), mainly via its antagonistic action on DKK2. These effects are not observed in DKK2 -/- mice.
          Catalogue Number317701
          Brand Family Calbiochem®
          Synonyms9-Carboxy-3-(dimethyliminio)-6,7-dihydroxy-10-methyl-3H-phenoxazin-10-ium iodide
          References
          ReferencesLi, X., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 11402.
          Product Information
          FormBlack powder
          Hill FormulaC₁₆H₁₆I₂N₂O₅
          Chemical formulaC₁₆H₁₆I₂N₂O₅
          Hygroscopic Hygroscopic
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetLRP5/6
          Purity≥90% 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 Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          317701

          References

          Reference overview
          Li, X., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 11402.
          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.

          Revision25-November-2013 JSW
          Synonyms9-Carboxy-3-(dimethyliminio)-6,7-dihydroxy-10-methyl-3H-phenoxazin-10-ium iodide
          DescriptionAn enhanced in solution stable gallocyanine analog that directly and reversibly targets human LRP5/6 (low density lipoprotein-related protein 5/6), and disrupts its interaction with Dkk (Dickkopf) in a competitive manner. Shown to potently reverse DKK1/2/4-mediated inhibition of WNT3A-stimulated reporter gene activity (IC50 ~ 10 - 30 µM in in NIH 3T3 cells) with no effects on sFRP4-mediated inhibition of Wnt signaling. Blocks Dkk-2 - alkaline phosphatase binding to cells expressing LRP5 (IC50 = 1 µM in LRP5 transfected NIH 3T3 cells). Reduces blood glucose levels, improves glucose tolerance, and increases insulin sensitivity in type 2 diabetic mice (1.5 mg/kg, i.p. daily), mainly via its antagonistic action on DKK2. These effects are not observed in DKK2 -/- mice.
          FormBlack powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₆H₁₆I₂N₂O₅
          Structure formulaStructure formula
          Purity≥90% by HPLC
          SolubilityDMSO (10 mg/ml) or H₂ (2.5 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesLi, X., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 11402.