CAY10650cPLA2α inhibitor,highly potent CAS# 1233706-88-1 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1233706-88-1 | SDF | Download SDF |
| PubChem ID | 45102612 | Appearance | Powder |
| Formula | C28H25NO6 | M.Wt | 471.5 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 43 mg/mL (91.20 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-(2-methylpropanoyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]indole-5-carboxylic acid | ||
| SMILES | CC(C)C(=O)C1=CN(C2=C1C=C(C=C2)C(=O)O)CC(=O)COC3=CC=C(C=C3)OC4=CC=CC=C4 | ||
| Standard InChIKey | HTOJZPHWNDZOPQ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C28H25NO6/c1-18(2)27(31)25-16-29(26-13-8-19(28(32)33)14-24(25)26)15-20(30)17-34-21-9-11-23(12-10-21)35-22-6-4-3-5-7-22/h3-14,16,18H,15,17H2,1-2H3,(H,32,33) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM.
IC50 value: 12 nM
Target: cPLA2
CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor. It 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. Animals were anesthetized and sacrificed 15 days after application of cPLA2α inhibitors. Treatment with the AACOCF3 and CAY10650 had a profound effect on the severity and chronicity of keratitis. In addition, hamsters treated with AACOCF3 had significantly less severe keratitis as compared with CAY10650 group. References: | |||||
CAY10650 Dilution Calculator
CAY10650 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1209 mL | 10.6045 mL | 21.2089 mL | 42.4178 mL | 53.0223 mL |
| 5 mM | 0.4242 mL | 2.1209 mL | 4.2418 mL | 8.4836 mL | 10.6045 mL |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1209 mL | 4.2418 mL | 5.3022 mL |
| 50 mM | 0.0424 mL | 0.2121 mL | 0.4242 mL | 0.8484 mL | 1.0604 mL |
| 100 mM | 0.0212 mL | 0.106 mL | 0.2121 mL | 0.4242 mL | 0.5302 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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CAY10650 is a potent inhibitor of phospholipase A2 with IC50 value of 12 nM [1].
Phospholipase A2 (PLA2) are enzymes that release fatty acids from the second carbon group of glycerol. PLA2 are composed of four major families: secreted PLA2 (sPLA2), cytosolic Ca2+-dependent PLA2 (cPLA2), Ca2+-independent PLA2 (iPLA2) and platelet-activating factor acetylhydrolases (PAF-AH) [1].
In Chinese hamsters infected with A.castellanii-laden contact lenses, CAY10650 had a significant effect on the severity and chronicity of keratitis, which suggested that CAY10650 can be used as a therapeutic target in Acanthamoeba keratitis (AK). Histopathological examination showed that CAY10650 treated groups had very mild inflammation. In the corneal stroma, there was very few PMNs infiltration and milled stroma swelling. The corneal epithelium was normal [1].
Reference:
[1]. Tripathi T, Abdi M, Alizadeh H. Role of phospholipase A₂ (PLA₂) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis. Exp Eye Res, 2013, 113: 182-191.
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Role of phospholipase A(2) (PLA(2)) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis.[Pubmed:23792108]
Exp Eye Res. 2013 Aug;113:182-91.
The aim of this study is to determine if the mannose-induced protein (MIP-133) from Acanthamoeba castellanii trophozoites induces apoptosis of corneal epithelial cells through a cytosolic phospholipase A2alpha (cPLA2alpha)-mediated pathway. The efficacy of cPLA2alpha inhibitors to provide protection against Acanthamoeba keratitis was examined in vivo. Chinese hamster corneal epithelial (HCORN) cells were incubated with or without MIP-133. MIP-133 induces significant increase in cPLA2alpha and macrophage inflammatory protein-2 (MIP-2/CXCL2) levels from corneal cells. Moreover, cPLA2alpha inhibitors, MAFP (Methyl-arachidonyl fluorophosphonate) and AACOCF3 (Arachidonyl trifluoromethyl ketone), significantly reduce cPLA2alpha and CXCL2 from these cells (P < 0.05). Additionally, cPLA2alpha inhibitors significantly inhibit MIP-133-induced apoptosis in HCORN cells (P < 0.05). Subconjunctival injection of purified MIP-133 in Chinese hamster eyes induced cytopathic effects resulting in corneal ulceration. Animals infected with A. castellanii-laden contact lenses and treated with AACOCF3 and CAY10650, showed significantly less severe keratitis as compared with control animals. Collectively, the results indicate that cPLA2alpha is involved in MIP-133 induced apoptosis of corneal epithelial cells, polymorphonuclear neutrophil infiltration, and production of CXCL2. Moreover, cPLA2alpha inhibitors can be used as a therapeutic target in Acanthamoeba keratitis.
