Triflusal

Modify Date: 2024-01-04 06:27:34

Triflusal Structure
Triflusal structure
Common Name Triflusal
CAS Number 322-79-2 Molecular Weight 248.155
Density 1.4±0.1 g/cm3 Boiling Point 316.0±42.0 °C at 760 mmHg
Molecular Formula C10H7F3O4 Melting Point 115 °C
MSDS Chinese USA Flash Point 144.9±27.9 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of Triflusal


Triflusal irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.Target: COXTriflusal at 10 mM, 100 mM and 1 M decreases LDH efflux in rat brain slices after anoxia/reoxygenation by 24%, 35% and 49% respectively. Triflusal also reduces inducible NO synthase activity by 18%, 21% and 30% [1].Triflusal (10 mg/kg i.v.) reduces platelet deposition on subendothelium-induced primary thrombus by about 68% in rabbits. Triflusal (10 mg/kg i.v.) reduces platelet deposition on a fresh thrombus formed over tunica media by about 48% in rabbits. Triflusal (40 mg/kg p.o.) reduces platelet deposition on a primary thrombus triggered by subendothelium and tunica media by 53% in rabbits. Triflusal (40 mg/kg p.o.) significantly reduces Cox-2 mRNA levels and protein levels without influence Cox-1 mRNA levels on the vascular wall in rabbits [2]. Triflusal (600 mg/day for 5 days) results in an increase in NO production by neutrophils and an increase in endothelial nitric oxide synthase (eNOS) protein expression in neutrophils in healthy volunteers [3].

 Names

Name 2-acetyloxy-4-(trifluoromethyl)benzoic acid
Synonym More Synonyms

 Triflusal Biological Activity

Description Triflusal irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.Target: COXTriflusal at 10 mM, 100 mM and 1 M decreases LDH efflux in rat brain slices after anoxia/reoxygenation by 24%, 35% and 49% respectively. Triflusal also reduces inducible NO synthase activity by 18%, 21% and 30% [1].Triflusal (10 mg/kg i.v.) reduces platelet deposition on subendothelium-induced primary thrombus by about 68% in rabbits. Triflusal (10 mg/kg i.v.) reduces platelet deposition on a fresh thrombus formed over tunica media by about 48% in rabbits. Triflusal (40 mg/kg p.o.) reduces platelet deposition on a primary thrombus triggered by subendothelium and tunica media by 53% in rabbits. Triflusal (40 mg/kg p.o.) significantly reduces Cox-2 mRNA levels and protein levels without influence Cox-1 mRNA levels on the vascular wall in rabbits [2]. Triflusal (600 mg/day for 5 days) results in an increase in NO production by neutrophils and an increase in endothelial nitric oxide synthase (eNOS) protein expression in neutrophils in healthy volunteers [3].
Related Catalog
Target

COX-2:280 μM (IC50)

COX-2:160 μM (IC50, in human blood)

References

[1]. Fernández de Arriba A, et al. Inhibition of cyclooxygenase-2 expression by 4-trifluoromethyl derivatives of salicylate, triflusal, and its deacetylated metabolite, 2-hydroxy-4-trifluoromethylbenzoic acid. Mol Pharmacol. 1999 Apr;55(4):753-60.

[2]. Duran, X., et al., Protective effects of triflusal on secondary thrombus growth and vascular cyclooxygenase-2. J Thromb Haemost, 2008. 6(8): p. 1385-92.

[3]. De Miguel, L.S., et al., A 4-trifluoromethyl derivative of salicylate, triflusal, stimulates nitric oxide production by human neutrophils: role in platelet function. Eur J Clin Invest, 2000. 30(9): p. 811-7.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 316.0±42.0 °C at 760 mmHg
Melting Point 115 °C
Molecular Formula C10H7F3O4
Molecular Weight 248.155
Flash Point 144.9±27.9 °C
Exact Mass 248.029648
PSA 63.60000
LogP 2.90
Vapour Pressure 0.0±0.7 mmHg at 25°C
Index of Refraction 1.484
Storage condition 2-8°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
GP4250000
CHEMICAL NAME :
2,4-Cresotic acid, alpha,alpha,alpha-trifluoro-, acetate
CAS REGISTRY NUMBER :
322-79-2
BEILSTEIN REFERENCE NO. :
2945374
LAST UPDATED :
199612
DATA ITEMS CITED :
5
MOLECULAR FORMULA :
C10-H7-F3-O4
MOLECULAR WEIGHT :
248.17
WISWESSER LINE NOTATION :
FXFFR DVQ COV1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
402 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: 3,225,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
217 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: 3,225,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
228 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: 3,225,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
437 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: 3,225,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
380 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: 3,225,1978

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H315-H317-H319-H335
Precautionary Statements P261-P280-P305 + P351 + P338
Hazard Codes Xn
Risk Phrases 22-36/37/38-43
Safety Phrases 26-36/37
RIDADR NONH for all modes of transport
RTECS GP4250000
HS Code 2918990090

 Customs

HS Code 2918990090
Summary 2918990090. other carboxylic acids with additional oxygen function and their anhydrides, halides, peroxides and peroxyacids; their halogenated, sulphonated, nitrated or nitrosated derivatives. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

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 Synonyms

Triflusal
2-(acetyloxy)-4-(trifluoromethyl)benzoic acid
α,α,α-Trifluoro-2,4-cresotic Acid Acetate
2-Acetoxy-4-trifluoromethylbenzoic acid
EINECS 206-297-5
Triflusalum [INN-Latin]
2-Acetoxy-4-trifluoromethylbenzoicacid
Benzoic acid, 2-(acetyloxy)-4-(trifluoromethyl)-
Triflusal [INN]
2-Acetoxy-4-trifluormethyl-benzoesaeure
2-Acetoxy-4-(trifluoromethyl)benzoic acid
2-Acetyloxy-4-trifluoromethylbenzoic acid
UR 1501
MFCD00866793
Disgren
Triflux
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  • DC Chemicals Limited
  • China
  • Product Name: Triflusal
  • Price: $400.0/100mg $800.0/250mg $1600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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Price: $79/10mM*1mLinDMSO

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