| Identification | Back Directory | [Name]
CAY10606 | [CAS]
1159576-98-3 | [Synonyms]
CAY10606
2-[(3-Chlorophenyl)methyl]-5-hydroxy-1H-benz[g]indole-3-carboxylic acid, ethyl ester | [Molecular Formula]
C22H18ClNO3 | [MDL Number]
MFCD18382112 | [MOL File]
1159576-98-3.mol | [Molecular Weight]
379.84 |
| Chemical Properties | Back Directory | [Melting point ]
222 °C(Solv: ethyl acetate (141-78-6); cyclohexane (110-82-7)) | [Boiling point ]
624.2±55.0 °C(Predicted) | [density ]
1.355±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 25 mg/ml; DMSO: 25 mg/ml; Ethanol: 20 mg/ml | [form ]
A crystalline solid | [pka]
8.86±0.30(Predicted) |
| Hazard Information | Back Directory | [Description]
5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs) from arachidonic acid, primarily in certain leukocyte populations. CAY10606 is a potent, reversible inhibitor of 5-LO, both in cell-free assays (IC50 = 86 nM) and in intact neutrophils (IC50 = 230 nM).1 It prevents the production of LTs in whole blood, whether 5-LO is activated with the calcium ionophore A23187 (IC50 = 1.6 μM) or formyl peptide (fMLP) following priming with lipopolysaccharide (IC50 = 830 nM). In rats subjected to carrageenan-induced pleurisy, CAY10606 significantly reduces both LT biosynthesis and the inflammatory reaction.1 | [Uses]
5-LOX-IN-6 (compound 11a) is a direct and reversible inhibitor of 5-lipoxygenase (5-LO). 5-LOX-IN-6 inhibits 5-LO activity in human neutrophils and recombinant human 5-LO with IC50 values of 0.23 and 0.086 μM, respectively. 5-LOX-IN-6 prevents leukotriene biosynthesis. 5-LOX-IN-6 can be used for inflammatory and allergic disorders research[1]. | [in vivo]
5-LOX-IN-6 (compound 11a) (4 mg/kg, ip) significantly prevents leukotriene B4 production in pleural exudates of λ-carrageenan (HY-N9470)-treated rats, associated with reduced severity of pleurisy[1]. | Animal Model: | Male Wistar Han rats (220-230 g, n=10 per group)[1] | | Dosage: | 4 mg/kg | | Administration: | IP, 30 min before λ-carrageenan administration. Rats were anaesthetized and λ-carrageenan (HY-N9470) was injected into the pleural cavity. | | Result: | significantly reduced the inflammatory reaction measured as exudate volume (77%),
inflammatory cell numbers (40%), and LTB4 levels (49%) in the pleural exudates. |
| [IC 50]
5-LO; LTB4 | [storage]
Store at -20°C | [References]
1. Karg, E.M., Luderer, S., Pergola, C., et al. Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase J. Med. Chem. 52,3474-3483(2009). |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|