Opn4 Antagonist – CAS 457961-34-1 – Calbiochem

Descrição detalhada : A 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., A 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.
Sinónimos : Opn4 Antagonist - CAS 457961-34-1 - Calbiochem; Opn4 Antagonist, Opsinamide, Melanopsin-inhibiting Sulfonamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine, Melanopsin Antagonist, Opsinamide AA92593
Fórmula molecula r: C13H19NO3S
Armazenamento : 2-8C; 2-8C
Embalagem : 1X1EA