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Triflusal

Pharmacological Study

Triflusal

CAS No.322-79-2
Chemical Name:Triflusal
CBNumber:CB9446472
Molecular Formula:C10H7F3O4
Formula Weight:248.16
MOL File:322-79-2.mol

Triflusal Property

Melting point 120-122° (upon slow heating); 110-112° (upon quick heating)
Boiling point 316.0±42.0 °C(Predicted)
Density 1.433±0.06 g/cm3(Predicted)
storage temp. Sealed in dry,2-8°C
solubility DMSO: >30mg/mL
pka 2.97±0.10(Predicted)
form powder
color white to off-white
λmax 297nm(H2O)(lit.)
Merck 14,9688
CAS DataBase Reference 322-79-2(CAS DataBase Reference)
FDA UNII 1Z0YFI05OO
ATC code B01AC18
UNSPSC Code 41116107
NACRES NA.25

Safety

Hazard Codes :Xn
Risk Statements :22-36/37/38-43
Safety Statements :26-36/37
WGK Germany :3
RTECS :GP4250000
HS Code :2918.29.7500

NFPA 704:

	0
2		0

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordWarning
Hazard statements H302-H315-H317-H319-H335
Precautionary statements P261-P264-P280-P280-P304+P340+P312-P333+P313

Triflusal Price More Price(3)

Brand: Sigma-Aldrich(India)
Product number: T6580
Product name : Triflusal
Purity: ≥98% (HPLC), powder
Packaging: 5MG
Price: ₹12427.1
Updated: 2022/06/14
Buy: Buy

Brand: TCI Chemicals (India)
Product number: T3601
Product name : Triflusal
Purity: min. 96.0 %
Packaging: 250MG
Price: ₹7700
Updated: 2022/05/26
Buy: Buy

Brand: TCI Chemicals (India)
Product number: T3601
Product name : Triflusal
Purity: min. 96.0 %
Packaging: 1G
Price: ₹9800
Updated: 2022/05/26
Buy: Buy

Triflusal Chemical Properties,Usage,Production

Pharmacological Study Triflusal is an antiplatelet agent structurally related to the salicylates, but it is not derived from ASA. Triflusal and its metabolite (3-hydroxy-4-triuoro-methylbenzoic acid or HTB) produce specific inhibition of platelet arachidonic acid metabolism (McNeely and Goa, 1998). A single 12-month open-label trial of tritriflusal in 73 VaD patients (López-Pousa et al., 1997) showed fewer declines in MMSE scores in the active group compared with untreated subjects. More recently, triusal was used in patients with amnesic MCI; 257 patients were randomized to receive 900 mg of triflusal or placebo for 18 months. Triflusal therapy was associated with a signicantly lower rate of conversion to dementia (Gómez-Isla et al., 2008).
Description Triflusal is an antiplatelet agent structurally related to the salicylates, but it is not derived from ASA. Triflusal and its metabolite (3-hydroxy-4-triuoro-methylbenzoic acid or HTB) produce specic inhibition of platelet arachidonic acid metabolism (McNeely and Goa, 1998). A single 12-month open-label trial of Triflusal in 73 VaD patients (López-Pousa et al., 1997) showed fewer declines in MMSE scores in the active group compared with untreated subjects. More recently, Triflusal was used in patients with amnesic MCI; 257 patients were randomized to receive 900 mg of Triflusal or placebo for 18 months. Triflusal therapy was associated with a signicantly lower rate of conversion to dementia (Gómez-Isla et al., 2008).
Chemical Properties White to Off-White Solid
Uses An analog of Aspirin; inhibits platelet aggregation. Antithrombotic.
Uses Antithrombotic;Cyclooxygenase inhibitor
Definition ChEBI: 2-acetyloxy-4-(trifluoromethyl)benzoic acid is a member of salicylates, a carboxylic ester and a member of benzoic acids.
Mechanism of action 2-hydroxy-4-trifluoromethylbenzoic acid (HTB), the deacetylated metabolite of triflusal, retains significant antiplatelet activity. Triflusal is rapidly absorbed and metabolized. The area under the concentration–time curve for triflusal is 20.26 mg/L/hour after a 900-mg dose, whereas that for HTB is 42.27 mg/L/hour. Much of the pharmacokinetic data for triflusal activity is associated with HTB. The inhibition of COX, as measured by reduced production of thromboxane B2, is 25% after 2 hours and 85% after 7 days with triflusal, whereas the effects of aspirin on thromboxane B2 is more than 90% reduction after 2 hours and is maintained at this level after 7 days. It would appear that the presence of a 4-trifluoromethyl group also greatly enhances triflusal's ability to inhibit the activation of nuclear factor κB, which in turn regulates the expression of the mRNA of vascular cell adhesion molecule-1 needed for platelet aggregation. In addition, triflusal increases nitric oxide synthesis in neutrophils, which results in an increased vasodilatory potential. Finally, an additional site of action for triflusal/HTB is the inhibition of cAMP phosphodiesterase, leading to increased levels of cAMP. Elevated cAMP levels decrease platelet aggregation through decreased mobilization of calcium. Aspirin and salicylic acid do not significantly increase cAMP levels.
Clinical Use Triflusal (2-acetoxy-4-trifluoromethyl benzoic acid) is an antiplatelet drug that despite its structural similarity to aspirin exhibits quite different pharmacological and pharmacokinetic properties.