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

Prevents melanopsin/Opn4 photoactivation in a reversible manner. Inhibits cellular phototransduction mediated by human Opn4 (IC₅₀ = 665 nM; using CHO transfectants).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Opn4 Antagonist, Opsinamide, Melanopsin-inhibiting Sulfonamide AA92593, Melanopsin Antagonist, Opsinamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine

Primary Target: melanopsin (Opn4)
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
457961-34-1C₁₃H₁₉NO₃S

Products

Catalog NumberPackaging Qty/Pack
5.09267.0001 Glass bottle 10 mg
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®
SynonymsOpn4 Antagonist, Opsinamide, Melanopsin-inhibiting Sulfonamide AA92593, Melanopsin Antagonist, Opsinamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine
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
Quality LevelMQ100
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
Global Trade Item Number
Catalog Number GTIN
5.09267.0001 04055977241747

Documentation

Opn4 Antagonist - CAS 457961-34-1 - Calbiochem 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
SynonymsOpn4 Antagonist, Opsinamide, Melanopsin-inhibiting Sulfonamide AA92593, Melanopsin Antagonist, Opsinamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine
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 Protect from light
+2°C to +8°C
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.