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Darbufelone Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5752984

Darbufelone is a dual inhibitor of cellular PGF2alpha and LTB4 production. Dabfilon effectively inhibited PGHS-2 (IC50 = 0.19 uM), but had a much smaller effect on PGHS-1 (IC50 = 20uM). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Darbufelone, Inhibitor
Full Product Name
Darbufelone
Product Synonym Names
CI-1004
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
332.46
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
Formula
C18H24N2O2S
SMILES
O=C1N=C(N)S/C1=C\C2=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C2
CAS Number
139226-28-1
Target & IC50
PGHS-2: ic50 0.19uM
PGHS-1: ic50 20uM
In Vitro
Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Dabfilon has oral activity in animal models of inflammation and arthritis and does not cause ulcers. When the mice were treated with bufafenone at a dose of 80 mg/kg/day, the tumor volume decreased in a time-dependent manner. In contrast, the lower dose of bufafenone (20 or 40 mg/kg/day) did not show any significant inhibition of tumor weight. At necropsy, the tumor weight of the mice treated with bufafenone (80 mg/kg/day) was reduced by 30.2% compared to the control group.

Product References and Citations for Darbufelone, inhibitor

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.
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.
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.
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.

Other Notes

Small volumes of Darbufelone, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Darbufelone purchase

MBS5752984 is an inhibitor targeting Darbufelone.
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