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.
CAS Number: 457961-34-1
Molecular Weight: 269.36
Chemical Name: 1-((4-methoxy-3-methylphenyl)sulfonyl)piperidine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
AA92593 was used at 10 µM final concentration in various in vitro assays.
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.
- Jones KA, et al. Small-molecule antagonists of melanopsin-mediated phototransduction. (2013) Nat Chem Biol. 9(10):630-5.
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