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Darbufelone mesylate

Catalog No. T10960L CAS 139340-56-0

Synonyms: CI-1004 mesylate

Darbufelone mesylate (CI-1004 mesylate) inhibited PGF2α and LTB4 in cells. Darbufelone mesylate inhibited PGHS-2 with IC50 value of 0.19 μM and PGHS-1 with IC50 value of 20 μM.

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Darbufelone mesylate, CAS 139340-56-0

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5 mg	In stock	$ 122.00
10 mg	In stock	$ 198.00
25 mg	6-8 weeks	$ 455.00
50 mg	6-8 weeks	Inquiry

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Purity: 96.81%

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Description	Darbufelone mesylate (CI-1004 mesylate) inhibited PGF2α and LTB4 in cells. Darbufelone mesylate inhibited PGHS-2 with IC50 value of 0.19 μM and PGHS-1 with IC50 value of 20 μM.
Targets&IC50	PGHS1:20 μM, PGHS2:0.19 μM, H520:21μM, PGHS2:10±5 μM(Ki), A549 cells:20μM, PGHS2:0.98 ± 0.03μM(Kd)
In vitro	Darbufelone, a noncompetitive inhibitor of PGHS-2 with a Ki value of 10±5 μM, exhibits fluorescence quenching of PGHS-2 at 325 nm (λex=280 nm) with a Kd of 0.98±0.03 μM[2]. To assess the putative anti-proliferative effect of Darbufelone, A549, H520, and H460 cell lines derived from three distinct pathological subtypes of non-small cell lung cancer (NSCLC) (adenocarcinoma, squamous, and large cell lung cancer, respectively) are utilized. The cell lines are treated with increasing concentrations of Darbufelone, ranging from 5 to 60 μM, for a duration of 72 hours. The growth inhibition of these three cell lines gradually increases with higher concentrations of the drug. The IC50 values for A549 and H520 are 20±3.6 and 21±1.8 μM, respectively, while H460 exhibits a lower IC50 of 15±2.7 μM[1].
In vivo	Darbufelone, a dual inhibitor of cellular PGF2R and LTB4 production, exhibits oral activity in animal models of inflammation and arthritis without causing ulcers. When mice were treated with bufafenone at a dose of 80 mg/kg/day, the tumor volume decreased in a time-dependent manner. In contrast, lower doses of bufafenone (20 or 40 mg/kg/day) did not significantly inhibit tumor weight. At necropsy, the tumor weight of mice treated with bufafenone (80 mg/kg/day) was reduced by 30.2% compared to the control group.

Synonyms	CI-1004 mesylate
Molecular Weight	428.57
Formula	C19H28N2O5S2
CAS No.	139340-56-0

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (233.33 mM), Sonification is recommended.

H2O: <0.1mg/mL

References and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library

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Keywords

Darbufelone mesylate 139340-56-0 GPCR/G Protein Immunology/Inflammation LTR Prostaglandin Receptor CI 1004 Mesylate Darbufelone Mesylate CI1004 Mesylate CI-1004 Mesylate CI-1004 mesylate inhibitor inhibit

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