Description
| 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.
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