| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| ln Vitro |
Competitive melanopsin antagonist AA92593 induces retinal displacement in the melanopsin binding site, which in turn sets off downstream signaling and finally results in elevated Per1 expression [1]. Due to its competition with retinal for the melanopsin retinal binding site—which is distinct from that of other opsins—AA92593 exhibits specificity [1]. The embryo becomes darker when AA92593, which inhibits melanopsin function, boosts a-MSH expression and causes melanin dispersion in melanocytes [3]. In CHOOpn4 cells, AA92593's IC50 is 665 nM [4].
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| ln Vivo |
In rabbits with normal lighting, AA92593 can lower intraocular pressure [2]. IOP lowers when melatonin levels are raised by AA92593 [2].
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| Cell Assay |
Cell viability assay[1]
Cell Types: Melan-a melanocytes and B16-F10 melanoma cells[1]. Tested Concentrations: 10μM. Incubation Duration: 1 hour (heated to 39.5 °C). Experimental Results: Pharmacological inhibition of melanopsin. |
| Animal Protocol |
Animal/Disease Models: wild-type (WT) mice [4].
Doses: 30 mg/kg. Route of Administration: Perform IP 20 minutes before PLR measurement. Experimental Results: Pupil contraction in response to light (1013 ph.cm−2.s−1) was diminished by approximately 50%. |
| 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. |
| Molecular Formula |
C13H19NO3S
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|---|---|
| Molecular Weight |
269.359
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| CAS # |
457961-34-1
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| SMILES |
COC1=CC=C(S(N2CCCCC2)(=O)=O)C=C1C
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| Chemical Name |
1-(4-Methoxy-3-methyl-benzenesulfonyl)-piperidine
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| Synonyms |
Cy-1001 Cy1001 Cy 1001AA-92593AA92593 AA 92593
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~928.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7125 mL | 18.5625 mL | 37.1250 mL | |
| 5 mM | 0.7425 mL | 3.7125 mL | 7.4250 mL | |
| 10 mM | 0.3713 mL | 1.8563 mL | 3.7125 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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