AA92593, Antagonist of Melanopsin-mediated Photo-transduction


Catalog No. size PriceQuantity
M60143-5S 5 mg solid $139
M60143-10S 10mg solid $299

Description

Product Information
Molecular Weight: 269.36
Formula: C13H19NO3S
Purity: ≥98%
CAS#: 457961-34-1
Solubility: DMSO up to 100 mM
Chemical Name: 1-((4-methoxy-3-methylphenyl)sulfonyl)piperidine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.


Biological Activity:


AA92593 is a potent and selective small molecule antagonist of melanopsin-mediated photo-transduction (IC50~160 nM). It inhibits melanopsin (opsinamides) by competing with retinal binding to melanopsin, and inhibits its function without affecting rod- and cone-mediated responses. In vivo administration of AA92593 to mice specifically and reversibly modified melanopsin-dependent light responses, including the pupillary light reflex and light aversion. Melanopsin, expressed in a subset of retinal ganglion cells, mediates behavioral adaptation to ambient light and other non-image-forming photic responses. The discovery of AA92593 raises the prospect of therapeutic control of the melanopsin photo-transduction system to regulate light-dependent behavior and remediate pathological conditions.


How to Use:


In vitro: AA92593 was used at 10 µM final concentration in various in vitro assays.

In vivo: AA92593 was dosed intraperitoneally 30 mg/kg 20 min before PLR measurement attenuated pupil constriction in response to light (1013 ph cm-2 s-1) by ~50% in adult rd mice.


Reference:


  • 1. Jones KA, et al. Small-molecule antagonists of melanopsin-mediated phototransduction. (2013) Nat Chem Biol. 9(10):630-5.



Products are for research use only. Not for human use.

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