| Identification | Back Directory | [Name]
CAY10650 | [CAS]
1233706-88-1 | [Synonyms]
CS-1520
CAY10650
CAY10650, >=98%
CAY 10650;CAY-10650
CAY10650;CAY-10650;CAY 10650
3-isobutanoyl-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]indole-5-carboxylic acid
3-(2-Methyl-1-oxopropyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid
1H-Indole-5-carboxylic acid, 3-(2-Methyl-1-oxopropyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C28H25NO6 | [MDL Number]
MFCD18206878 | [MOL File]
1233706-88-1.mol | [Molecular Weight]
471.5 |
| Chemical Properties | Back Directory | [Melting point ]
103-104℃ | [Boiling point ]
685.4±55.0 °C(Predicted) | [density ]
1.24±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 20 mg/ml; DMSO: 20 mg/ml; DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml | [form ]
Powder | [pka]
4.03±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process. 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. The phase I metabolite of this compound, CAY10641 , is also available. | [Uses]
CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM. CAY10650 suppresses lipid droplets formation and PGE2 secretion[1][2]. | [in vivo]
CAY10650 (50 μg/5 μL; Inject with topical eye-drop; Chinese hamsters) relieves acanthamoeba keratitis in vivo.[1]. | Animal Model: | Chinese hamsters with infected with parasite-laden contact lenses[1] | | Dosage: | 50 μg/5 μL | | 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 | | Result: | Reduced the severity of the keratitis and hasten the onset of resolution.
Had little mild inflammation and very few PMNs infiltration in the corneal stroma.
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| [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. DOI:10.1038/s41598-020-67345-3
[2] Tripathi T, et, al. Role of phospholipase A? (PLA?) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis. Exp Eye Res. 2013 Aug;113:182-91. DOI:10.1016/j.exer.2013.05.021 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
|