Opn4 Antagonist-CAS 457961-34-1-Calbiochem

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一般描述

A sulfonamide compound that prevents melanopsin/Opn4 photoactivation in a reversible andcis-Retinal-competitive manner (K_b= 6 and 0.16 ?M in competitive binding studies using Opn4 pre-bound withcis-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 ?M 9-cis-Retinal & photoactivation), by murine Opn4 in transfectedXenopusoocytes (IC₅₀= 190 nM; drug added 3 min before 50 ?M 11-cis-Retinal and photoactivation), as well as by endogenous Opn4 in primary rat ipRGCs (intrinsically photosensitive retinal ganglion cells; 10 ?M). Shown to be bioavailable in miceviai.p. injection (retina [AA92593] ~7.5 ?M 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 micein vivo. Likewise, blue light insensitivity is observed inOpn4^-/-and AA92593-treated wild-type, but not vehicle-treated wild-type, P14 neonatal mice.
A sulfonamide compound that prevents melanopsin/Opn4 photoactivation in a reversible andcis-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 transfectedXenopusoocytes), and rat Opn4 (10 ?M; 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 inOpn4^-/-and AA92593-treated wild-type, but not vehicle-treated wild-type, P14 neonatal mice.

生化/生理作用

Cell permeable: yes
Target K_i: 110 and 160 nM for human and mouse melanopsin, respectively)
Reversible: yes
Primary Target
melanopsin (Opn4)

包装

Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 monthst at -20°C.

其他说明

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

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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