131614-02-3

131614-02-3 structure
131614-02-3 structure
  • Name: E-​6123
  • Chemical Name: (+)-6-(2-chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido<4',3':4,5>thieno<3,2-f><1,2,4>triazolo<4,3-a><1,4>diazepine
  • CAS Number: 131614-02-3
  • Molecular Formula: C23H22ClN5OS
  • Molecular Weight: 451.97200
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2016-11-04 16:04:28
  • Modify Date: 2025-08-25 17:13:34
  • E-​6123 is a platelet-activating factor (PAF) receptor antagonist.

Name (+)-6-(2-chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido<4',3':4,5>thieno<3,2-f><1,2,4>triazolo<4,3-a><1,4>diazepine
Synonyms e-6123
Description E-​6123 is a platelet-activating factor (PAF) receptor antagonist.
Related Catalog
Target

PAF[1]

In Vitro 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].
Cell Assay 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].
References

[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.

Density 1.57g/cm3
Boiling Point 720.4ºC at 760 mmHg
Molecular Formula C23H22ClN5OS
Molecular Weight 451.97200
Flash Point 389.5ºC
Exact Mass 451.12300
PSA 91.62000
LogP 3.87080
Vapour Pressure 1.32E-20mmHg at 25°C
Index of Refraction 1.806

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UV1200278
CAS REGISTRY NUMBER :
131614-02-3
LAST UPDATED :
199612
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C23-H22-Cl-N5-O-S
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
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