AA92593 |
| Catalog No.GC61951 |
AA92593은 선택적이고 경쟁적인 OPN4(멜라놉신) 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 457961-34-1
Sample solution is provided at 25 µL, 10mM.
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AA92593 is a selective and competitive OPN4 (melanopsin) antagonist[1][2].
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[1].AA92593 is shown to be specific because it competes with retinaldehyde for the melanopsin retinal binding site which is very distinct from other opsins[1].Inhibition of melanopsin activity with AA92593 increases a-MSH expression and induces melanin dispersion in the melanophores, which darkens the embryo[3].AA92593 exhibits an IC50 of 665 nM in CHOOpn4 cells[4].
AA92593 is able to decrease IOP in rabbits living under normal light condition[2].AA92593 produces an increment in melatonin levels resulting in a drop of IOP[2].
References:
[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.
[3]. Gabriel E Bertolesi, et al. Melanopsin photoreception in the eye regulates light-induced skin colour changes through the production of α-MSH in the pituitary gland. Pigment Cell Melanoma Res. 2015 Sep;28(5):559-71.
[4]. Kenneth A Jones, et al. Small-molecule antagonists of melanopsin-mediated phototransduction. Nat Chem Biol. 2013 Oct;9(10):630-5.
| Cas No. | 457961-34-1 | SDF | |
| Canonical SMILES | O=S(N1CCCCC1)(C2=CC=C(OC)C(C)=C2)=O | ||
| Formula | C13H19NO3S | M.Wt | 269.36 |
| Solubility | DMSO : 250 mg/mL (928.13 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7125 mL | 18.5625 mL | 37.125 mL |
| 5 mM | 0.7425 mL | 3.7125 mL | 7.425 mL |
| 10 mM | 0.3713 mL | 1.8563 mL | 3.7125 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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