furaprofen

Modify Date: 2024-01-10 12:01:57

furaprofen Structure
furaprofen structure
Common Name furaprofen
CAS Number 67700-30-5 Molecular Weight 266.29100
Density 1.23g/cm3 Boiling Point 449.4ºC at 760 mmHg
Molecular Formula C17H14O3 Melting Point N/A
MSDS N/A Flash Point 225.6ºC

 Use of furaprofen


R803 is an effective HCV replication inhibitor. R803 is substantially more potent against genotype 1a and 1b replicons (EC50, ~30 nM) than against the genotype 2a replicon (EC50, ~1,000 nM).

 Names

Name furaprofen
Synonym More Synonyms

 furaprofen Biological Activity

Description R803 is an effective HCV replication inhibitor. R803 is substantially more potent against genotype 1a and 1b replicons (EC50, ~30 nM) than against the genotype 2a replicon (EC50, ~1,000 nM).
Related Catalog
Target

EC50: ~30 nM (HCV genotype 1a and 1b replicons), ~1000 nM (HCV genotype 2a replicon)[1]

In Vitro R803 is potent and highly specific for HCV replication. The antiviral activity of R803 has been determined by a reporter replicon assay with multiple repeats to be 29.88±8.05 nM, an ~3-fold improvement over the activity of the parent compound, R706. The potency of R803 against the replicon is also confirmed by both Western blotting and TaqMan RT-PCR to be about 37 nM and 54.67±4.11 nM, respectively . To assess the general effect of R803 on cell proliferation, a panel of primary cells and transformed human cell lines are treated with increasing doses of R803 for 48 h, and the effect on cell proliferation is measured by an MTS-based cell viability assay. The the concentration that caused a 50% reduction in cell numbers in the absence of virus infection (CC50) of R803 is found to range from 2 μM to ≥10 μM, depending on the cell type and proliferation status[1].
Kinase Assay Plasmid PV-Luc is linearized with the PvuI restriction enzyme and subjected to in vitro transcription using the RiboMAX Large Scale RNA Production System-T7. After DNase I digestion and purification, the transcribed RNA (5 μg) is electroporated into Huh-7 cells at 270 V and 950 μF on a Gene Pulser II system. The cells are then dispensed into white 96-well plates at a density of 10,000/90 μL/well. R803 is serially diluted in compound diluent (10% DMSO, 20% methanol) and added to each well in a volume of 10 μL. The plates are incubated for 18 h at 37°C under 5% CO2 before luciferase activity is determined using the Bright-Glo luciferase assay kit[1].
Cell Assay Replicon 9-13 cells are plated onto 6-well plates 24 h prior to the treatment. Serial dilutions of R803 are made in a mixture containing 90% of the culture medium, 7.2% 1× PBS, 1.8% methanol, 1% DMSO, 20 μM RBV, and varying concentrations of IFN-α for a fixed-ratio dose-response study. The cells are treated with the designated combinations of R803 (0 to 80 nM concentrations) and IFN-α (0 to 4 IU/mL) plus 20 μM RBV for 72 h; then they are washed with PBS, lysed in SDS loading buffer, and analyzed by Western blotting[1].
References

[1]. Huang P, et al. Discovery and characterization of substituted diphenyl heterocyclic compounds as potent and selective inhibitors of hepatitis C virus replication. Antimicrob Agents Chemother. 2008 Apr;52(4):1419-29.

 Chemical & Physical Properties

Density 1.23g/cm3
Boiling Point 449.4ºC at 760 mmHg
Molecular Formula C17H14O3
Molecular Weight 266.29100
Flash Point 225.6ºC
Exact Mass 266.09400
PSA 50.44000
LogP 4.28790
Index of Refraction 1.627

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DF6424000
CHEMICAL NAME :
7-Benzofuranacetic acid, alpha-methyl-3-phenyl-, (+-)-
CAS REGISTRY NUMBER :
67700-30-5
LAST UPDATED :
199109
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C17-H14-O3
MOLECULAR WEIGHT :
266.31
WISWESSER LINE NOTATION :
T56 BOJ DR& IY1&VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
5 mg/kg
TOXIC EFFECTS :
Gastrointestinal - other changes
REFERENCE :
JCPCBR Journal of Clinical Pharmacology. (Hall Assoc., PO Box 482, Stamford, CT 06904) V.13- 1973- Volume(issue)/page/year: 16,473,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
950 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 214,240,1975
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>1400 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 214,240,1975

 Synonyms

R803