509267 | Opn4 Antagonist - CAS 457961-34-1 - Calbiochem

509267
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₃H₁₉NO₃S 457961-34-1

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.09267.0001
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          Glass bottle 10 mg
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          Description
          OverviewA sulfonamide compound that prevents melanopsin/Opn4 photoactivation in a reversible and cis-Retinal-competitive manner without apparent affinity toward bovine retina rhodopsin or a panel of 74 other receptors, ion channels, and enzymes. Effectively inhibits cellular phototransduction mediated by human Opn4 (IC50 = 665 nM; using CHO transfectants), murine Opn4 (IC50 = 190 nM; using transfected Xenopus oocytes), and rat Opn4 (10 µM; using primary rat ipRGCs). Shown to effectively suppress PLR (pupillary light reflex; pupil constriction) in a time- and Opn4-dependent manner in mice (30 mg/kg i.p.) in vivo. Likewise, blue light insensitivity is observed in Opn4-/- and AA92593-treated wild-type, but not vehicle-treated wild-type, P14 neonatal mice.
          Catalogue Number509267
          Brand Family Calbiochem®
          SynonymsMelanopsin-inhibiting Sulfonamide AA92593, Melanopsin Antagonist, Opsinamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine, Opn4 Antagonist, Opsinamide
          References
          ReferencesJones, K.A., et al. 2013. Nat. Chem. Biol. 9, 630.
          Product Information
          CAS number457961-34-1
          FormWhite solid
          Hill FormulaC₁₃H₁₉NO₃S
          Chemical formulaC₁₃H₁₉NO₃S
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary Targetmelanopsin (Opn4)
          Primary Target K<sub>i</sub>110 and 160 nM for human and mouse melanopsin, respectively)
          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 Ambient Temperature Only
          Toxicity Regulatory Review
          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 6 monthst 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) 

          References

          Reference overview
          Jones, K.A., et al. 2013. Nat. Chem. Biol. 9, 630.
          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.

          Revision21-February-2014 JSW
          SynonymsMelanopsin-inhibiting Sulfonamide AA92593, Melanopsin Antagonist, Opsinamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine, Opn4 Antagonist, Opsinamide
          DescriptionA sulfonamide compound that prevents melanopsin/Opn4 photoactivation in a reversible and cis-Retinal-competitive manner (Kb = 6 and 0.16 µM in competitive binding studies using Opn4 pre-bound with cis-Retinal or not) without apparent affinity toward bovine retina rhodopsin or a panel of 74 other receptors, ion channels, and enzymes. Effectively inhibits cellular phototransduction mediated by human Opn4 in CHO transfectants (IC50 = 665 nM; drug added 30 min before 10 µM 9-cis-Retinal & photoactivation), by murine Opn4 in transfected Xenopus oocytes (IC50 = 190 nM; drug added 3 min before 50 µM 11-cis-Retinal and photoactivation), as well as by endogenous Opn4 in primary rat ipRGCs (intrinsically photosensitive retinal ganglion cells; 10 µM). Shown to be bioavailable in mice via i.p. injection (retina [AA92593] ~7.5 µM 30 min post 30 mg/kg i.p. dosing; >95% clearance within 2 h) and effectively suppress PLR (pupillary light reflex; pupil constriction) in a time- and Opn4-dependent manner in mice in vivo. Likewise, blue light insensitivity is observed in Opn4-/- and AA92593-treated wild-type, but not vehicle-treated wild-type, P14 neonatal mice.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number457961-34-1
          Chemical formulaC₁₃H₁₉NO₃S
          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 6 monthst at -20°C.
          Toxicity Regulatory Review
          ReferencesJones, K.A., et al. 2013. Nat. Chem. Biol. 9, 630.