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25mg |
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Purity: ≥98%
CAY10650 (CAY-10650) is a novel and highly potent inhibitor of cytosolic phospholipase A2α (cPLA2α) (IC50 = 12 nM) with anti-inflammatory activity. cPLA2α is involved in MIP-133 induced apoptosis of corneal epithelial cells, polymorphonuclear neutrophil infiltration, and production of CXCL2. Moreover, cPLA2α inhibitors can be used as a therapeutic target in Acanthamoeba keratitis. CAY10650 demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis. Chinese hamsters (n = 6/group) were infected with parasite-laden contact lenses and treated with cPLA2α inhibitors (AACOCF3 and CAY10650) 50 μg/5 μl was injected with topical eye-drop under the contact lens of an infected cornea three times a day for 6 days and topically on days 7–14 postinfection.Treatment with the AACOCF3 and CAY10650 had a profound effect on the severity and chronicity of keratitis.
ln Vitro |
Neutrophils treated with CAY10650 (12 nM; 30 min) exhibit inhibition of phosphorylated cPLA2-α (p-cPLA2-α) expression[1]. PGE2 release in neutrophils is inhibited by CAY10650 (12 nM; 2 h)[1].
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ln Vivo |
In vivo acanthamoeba keratitis is relieved by CAY10650 (50 μg/5 μL; inject with topical eye-drop; Chinese hamsters)[1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: Neutrophils Tested Concentrations: 12 nM Incubation Duration: 30 minutes Experimental Results: Inhibited cPLA2-α and inhibited the expression of the p-cPLA2-α. Western Blot Analysis[1] Cell Types: Neutrophils Tested Concentrations: 12 nM Incubation Duration: 2 hrs (hours) Experimental Results: Inhibited the PGE2 secretion and inhibited PGE2 realease. |
Animal Protocol |
Animal/Disease Models: Chinese hamsters with infected with parasite-laden contact lenses[1]
Doses: 50 μg/5 μL Route of Administration: Inject with topical eye-drop under the contact lens; three times a day for 6 days and topically on days 7 to 20 postinfection Experimental Results: decreased the severity of the keratitis and hasten the onset of resolution. Had little mild inflammation and very few PMNs infiltration in the corneal stroma. |
References |
[1]. Paloschi MV, et, al. Cytosolic phospholipase A2-α participates in lipid body formation and PGE2 release in human neutrophils stimulated with an L-amino acid oxidase from Calloselasma rhodostoma venom. Sci Rep. 2020 Jul 3;10(1):10976.
[2]. Tripathi T, et, al. Role of phospholipase A₂ (PLA₂) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis. Exp Eye Res. 2013 Aug;113:182-91. |
Molecular Formula |
C28H25NO6
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Molecular Weight |
471.5
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CAS # |
1233706-88-1
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Related CAS # |
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(C1=CC2=C(N(CC(COC3=CC=C(OC4=CC=CC=C4)C=C3)=O)C=C2C(C(C)C)=O)C=C1)O
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.30 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 25.0 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: ≥ 2.5 mg/mL (5.30 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 25.0 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: ≥ 2.5 mg/mL (5.30 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 | 2.1209 mL | 10.6045 mL | 21.2089 mL | |
5 mM | 0.4242 mL | 2.1209 mL | 4.2418 mL | |
10 mM | 0.2121 mL | 1.0604 mL | 2.1209 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.
Chinese hamsters (n = 9/group) were infected with parasite-laden contact lenses as described earlier.cPLA2αinhibitors (AACOCF3 and CAY10650) 50 μg/5μl was injected under the contact lens of an infected cornea three times a day for 6 days and topically on days 7 to 20 post-infection.Exp Eye Res.2013 Aug;113:182-91. th> |
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Photomicrograph of corneas from a Chinese hamster infected withAcanthamoebatrophozoites-laden contact lenses. cPLA2αinhibitors (AACOCF3 and CAY10650) 50 μg/5 μl was injected under the contact lens of an infected cornea three times a day for 6 days and topically from 7 to 14 days post-infection.Exp Eye Res.2013 Aug;113:182-91. td> |