AA92593 是选择性、竞争性的的 OPN4 (melanopsin) 拮抗剂。

AA92593 is a selective and competitive OPN4 (melanopsin) antagonist.

Solid

AA92593 is a competitive melanopsin antagonist, its presence in the retinal-binding pocket of melanopsin leads to the displacement of retinal, which could trigger a downstream signaling that would ultimately result in Per1 increased expression.
AA92593 is shown to be specific because it competes with retinaldehyde for the melanopsin retinal binding site which is very distinct from other opsins.
Inhibition of melanopsin activity with AA92593 increases a-MSH expression and induces melanin dispersion in the melanophores, which darkens the embryo.
AA92593 exhibits an IC50 of 665 nM in CHO cells.
has not independently confirmed the accuracy of these methods. They are for reference only.

AA92593 is able to decrease IOP in rabbits living under normal light condition.
AA92593 produces an increment in melatonin levels resulting in a drop of IOP.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Maria Nathália Moraes, et al. Melanopsin, a Canonical Light Receptor, Mediates Thermal Activation of Clock Genes. Sci Rep. 2017 Oct 25;7(1):13977.
[2]. Victoria Eugenia Lledó, et al. Yellow Filter Effect on Melatonin Secretion in the Eye: Role in IOP Regulation. Curr Eye Res. 2019 Jun;44(6):614-618.

In Vitro: DMSO : 250 mg/mL (928.13 mM; Need ultrasonic)配制储备液