371825 | GPCR-Helix 8 Signaling Inhibitor, JF5 - Calbiochem

371825
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₂₂N₂ • HI

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      371825-10MG
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      Stocked 
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      Available
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable quinolinimine compound that acts as a selective, potent blocker of G-protein coupled receptors (GPCR) that contain a constrained eighth helix (H8). The inhibition is selective and blocks G-protein signaling mediated via Gαq, but not Gα12. A non-orthosteric antagonist of PAR1 (IC50 = 4 µM) that is shown to inhibit PAR1 and CCR-4 induced platelet aggregation without affecting PAR4 mediated aggregation. Shown to inhibit thrombus formation following vascular injury (IC50 ~1 mg/kg). Also acts as a potent, non-competitive blocker of α2A-adrenergic receptors (IC50 = 2.5 µM as shown by a decrease in 3H-yohimbine binding).
          Catalogue Number371825
          Brand Family Calbiochem®
          Synonyms4-Pentyl-2,3-dihydro-1H-cyclopenta[b]quinolin-9-imine, HI, 4-Pentyl-1,2,3,4-tetrahydro-9H-cyclopenta[b]quinolin-9-imine, HI, GPCR-H8 Signaling Inhibitor, JF5
          References
          ReferencesDowal, L., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 2951.
          Product Information
          FormOff-white powder
          Hill FormulaC₁₇H₂₂N₂ • HI
          Chemical formulaC₁₇H₂₂N₂ • HI
          Hygroscopic Hygroscopic
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥92% 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
          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
          371825

          References

          Reference overview
          Dowal, L., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 2951.
          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.

          Revision24-August-2012 JSW
          Synonyms4-Pentyl-2,3-dihydro-1H-cyclopenta[b]quinolin-9-imine, HI, 4-Pentyl-1,2,3,4-tetrahydro-9H-cyclopenta[b]quinolin-9-imine, HI, GPCR-H8 Signaling Inhibitor, JF5
          DescriptionA cell-permeable quinolinimine compound that acts as a selective, potent blocker of G-protein coupled receptors (GPCR) that contain a constrained eighth helix (H8). The inhibition is selective and blocks G-protein signaling mediated via Gαq, but not Gα12. A non-orthosteric antagonist of PAR1 (IC50 = 4 µM) that is shown to inhibit PAR1 and CCR-4 induced platelet aggregation without affecting PAR4 mediated aggregation. Shown to inhibit thrombus formation following vascular injury (IC50 ~1 mg/kg). Also acts as a potent, non-competitive blocker of α2A-adrenergic receptors (IC50 = 2.5 µM as shown by a decrease in 3H-yohimbine binding).
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₇H₂₂N₂ • HI
          Structure formulaStructure formula
          Purity≥92% by HPLC
          SolubilityDMSO (50 mg/ml)
          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
          ReferencesDowal, L., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 2951.