YC-001 |
Katalog-Nr.GC64384 |
YC-001 ist ein inverser Agonist und Antagonist von Rod Opsin.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 748778-73-6
Sample solution is provided at 25 µL, 10mM.
YC-001 is a non-retinal compound that has been revealed to have both inverse agonist and antagonist activity toward rod opsin [1]. Cell-based β-Gal fragment complementation activity of YC-001 (EC50: 8.7µM) showed a potency of 7.8 µM and an efficacy at 150-310% of the control activity score [1].
YC-001 (0.5, 1, 5, 10, 20, 40 µM) improves the glycosylation profile of P23H opsin mutant [1]. YC-001 (0,-1.5 µM) reversibly binds rod opsin with EC50 of 0.98 µM [1]. YC-001 (0.313, 0.625, 1.25, 2.5, 5, 10, 20, 80 µM) increases in cAMP level in a dose-dependent manner in NIH3T3 cells [1]. YC-001 rescued multiple of 27 adRP-causing RHO mutants to NIH3T3 cells. 9-cis-retinal, F5257-0462, and YC-001 rescued cell surface transport of 16, 11, and 7 mutants, respectively [2].
YC-001(40 µM, 48 h) increases the percentage of ciliary targeted RHOP23H primarily by decreasing the level of misfolded RhoP23H mutant in the ONL, which is contributed by reduced total RHOP23H protein load [2]. YC-001 improves RHO protein quality and proteostasis of the RhoP23H/+ retinae [2].YC-001 showed a TC50 (the toxic concentration of a chemical that causes the cells growing 50% as well as control) at 202 µM in RhoP23H/+ retinal explants and 64 µM in WT retinae [2].
YC-001(50 or 200 mg kg-1, i.p. )protects Abca4-/-Rdh8-/- mice from bright light-induced retinal degeneration [1].About 70 pmol per eye of YC-001 was detected at 0.5 h after i.p. injection at 200 mg kg-1 bw, increasing to 280 pmol per eye at 3 h, and then diminishing to an undetectable level by 24 h [1].YC-001 showed fast ocular clearance with a t1/2 at 0.68 hours [2].
References:
[1]:Chen Y, Chen Y, Jastrzebska B, et al. A novel small molecule chaperone of rod opsin and its potential therapy for retinal degeneration[J]. Nature communications, 2018, 9(1): 1-18.
[2]:Vats A, Xi Y, Feng B, et al. Nonretinoid chaperones improve rhodopsin homeostasis in a mouse model of retinitis pigmentosa[J]. JCI insight, 2022, 7(10).
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