| Identification | Back Directory | [Name]
(5Z)-2-Amino-5-[(4-hydroxy-3,5-ditert-butyl-phenyl)methylidene]-1,3-thiazol-4-one | [CAS]
139226-28-1 | [Synonyms]
CS-490
darbufelone
5-((z)-3,5-di-tert-butyl-4-hydroxybenzylidene)-2-imino-4-thiazolidinone
(Z)-2-AMino-5-(3,5-di-tert-butyl-4-hydroxybenzylidene)thiazol-4(5H)-one
(5Z)-2-amino-5-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one
(5z)-2-amino-5-[(4-hydroxy-3,5-ditert-butyl-phenyl)methylidene]-1,3-thiazol-4-one
4(5H)-Thiazolone, 2-amino-5-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-, (5Z)- | [EINECS(EC#)]
1312995-182-4 | [Molecular Formula]
C18H24N2O2S | [MOL File]
139226-28-1.mol | [Molecular Weight]
332.46 |
| Chemical Properties | Back Directory | [Boiling point ]
448.6±55.0 °C(Predicted) | [density ]
1.18±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
9.98±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM). | [Biological Activity]
Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production. It potently inhibits PGHS-2 (IC50=0.19 μM), but is much less potent against PGHS-1 (IC50=20 μM). | [in vivo]
Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis. | [target]
IC50: 0.19 μM (PGHS-2), 20 μM (PGHS-1) | [storage]
Store at -20°C | [References]
[1] Johnson AR, et al. Slow-binding inhibition of human prostaglandin endoperoxide synthase-2 with darbufelone, an isoform-selective antiinflammatory di-tert-butyl phenol. Biochemistry. 2001 Jun 26;40(25):7736-45. DOI:10.1021/bi002343f
[2] Ye X, et al. Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo. Cancer Chemother Pharmacol. 2010 Jul;66(2):277-85. DOI:10.1007/s00280-009-1161-z |
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| Company Name: |
LGM Pharma
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| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
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