E-​6123

E-​6123 is a platelet-activating factor (PAF) receptor antagonist.

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

PAF[1]

E-6123 (E6123) partially inhibits the Thapsigargin-induced increase in the levels of interleukin-6 mRNA and interleukin-6 protein. To clarify the role of the concurrently produced cell-associated PAF in the thapsigargin-induced increase in the interleukin-6 mRNA level and interleukin-6 production, the effects of the PAF receptor antagonist E-6123 are examined. E-6123 at 1 and 10 μM partially inhibits the Thapsigargin (46.1 nM)-induced increase in the interleukin-6 mRNA level at 4 h and interleukin-6 production at 8 h[1].

The viability of the cells is examined in each set of experiments by a procedure using MTT, which is based on the ability of mitochondrial succinate dehydrogenase to cleave MTT to the blue compound formazan. After the peritoneal cells are incubated for the periods indicated in 10 mL of medium containing the various drugs (e.g., E-6123), 1 mL of MTT solution in phosphate-buffered saline (5 mg/mL, pH 7.4) is added to each dish, and the cells are further incubated for 4 h at 37 °C. Next, 2.5 mL of 0.04 N HCl solution in isopropanol is added, and the cells are sonicated at 10% maximum power for 3 s. The resultant colored product is read on a Microplate Reader at 570 nm[1].

[1]. Ichinowatari G, et al. Participation of prostaglandin E2 and platelet-activating factor in thapsigargin-induced production of interleukin-6. Eur J Pharmacol. 2002 Jan 11;434(3):187-96.

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

MOLECULAR WEIGHT :

452.01

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD - Lethal dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>500 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 16,310,1991

TYPE OF TEST :

LD - Lethal dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

>100 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 16,310,1991