| CAS NO: | 1233706-88-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 471.5 |
|---|---|
| Formula | C28H25NO6 |
| CAS No. | 1233706-88-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 43 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: | |
| 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 |
| Synonyms | CAY10650; CAY-10650; CAY 10650 |
| In Vitro | In vitro activity: CAY10650 is a novel and highly potent inhibitor of cytosolic phospholipase A2α (cPLA2α) with IC50 of 12 nM. 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 Kinase Assay: CAY10650 is a novel and highly potent inhibitor of cytosolic phospholipase A2α (cPLA2α) with IC50 of 12 nM. Cell Assay: |
|---|---|
| In Vivo | 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. |
| Animal model | Mouse model of acute irritant contact dermatitis. |
| Formulation & Dosage | 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. |
| References | Exp Eye Res. 2013 Aug;113:182-91. |
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