Cat. No.: HY-B0531

Triflusal

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Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.

For research use only. We do not sell to patients.

Purity: 99.56%
CAS No.: 322-79-2
Formula: C₁₀H₇F₃O₄
Molecular Weight:248.16

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Triflusal Chemical Structure

CAS No.: 322-79-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[4]

COX-1

NF-κB

iNOS

eNOS

All COX Isoforms :

All Phosphodiesterase (PDE) Isoforms :

All NF-κB Isoforms :

All NO Synthase Isoforms :

All Prostaglandin Receptor Isoforms :

In Vitro

Triflusal (37.5-300 μM; 30 min pre-incubation) does not significantly inhibit endothelial Cox-2 activity or reduce prostacyclin synthesis in Phorbol 12-myristate 13-acetate (HY-18739)-stimulated porcine aortic endothelial cells^[2].
Triflusal irreversibly inhibits COX-1 and reduces TXB₂ production in human platelets while sparing vascular endothelial cell arachidonic acid metabolism, and exhibits greater anti-aggregant potency in human whole blood than in platelet rich plasma^[3].
Triflusal increases NO production by human neutrophils by 150%, inhibits NF-κB activation in human mononuclear cells^[3].
Triflusal (3.3 mM) inhibits thrombin-induced platelet activation by 61% in human platelet-rich plasma^[4].
Triflusal (1 mM) increases basal cAMP levels by 36% in rat^[4].
Triflusal (3 mM) inhibits NF-κB activation in human peripheral blood mononuclear cells^[4].
Triflusal potently inhibits cAMP phosphodiesterase, significantly elevates cGMP levels in human platelets and neutrophils: it is ~2-fold more potent at inhibiting TNFα-induced NFκB activation, ~4-10-fold more potent at inhibiting NFAT-mediated transcription, and effective at attenuating anoxia/reperfusion-related injury, iNOS activity and lipid peroxidation in rat brain slices^[4].
Triflusal inhibits NF-κB activation and downstream expression of proinflammatory mediators in human peripheral blood mononuclear cells and endothelial cells, and strongly suppresses inflammation-induced COX-2 expression in human cells^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Triflusal (40 mg/kg/day; p.o.; daily; 8 days) reduces vascular Cox-2 mRNA and protein expression in normal rabbit aortas while sparing Cox-1 mRNA, with only a 39% reduction in Cox-2 protein levels^[2].
Triflusal (40 mg/kg/day; p.o.; daily; 8 days) reduces secondary platelet deposition on preformed primary thrombi in a rabbit model of severe carotid stenosis by 53-63% ^[2].
Triflusal (10 mg/kg; i.v.; single dose) reduces secondary platelet deposition on preformed primary thrombi in a rabbit model of thrombosis by 48-66%^[2].
Triflusal (chronic administration) provides 60% protection against arachidonic acid-induced cerebral ischaemia in rats^[3].
Triflusal (30 mg/kg) reduces NMDA (HY-17551)-induced excitotoxic brain lesions in rats^[3].
Triflusal inhibits neuronal and glial NF-κB activation, reduces lesion volume by approximately 50%, and dampens the astroglial response in a postnatal rat model of excitotoxic brain injury^[4].
Triflusal reduces inflammatory markers and functional deficits in rat models of isolated cerebral ischaemia or isolated Alzheimer's disease-like pathology, but has reduced efficacy in a model of concurrent cerebral ischaemia and Alzheimer's disease-like pathology^[4].
Triflusal (30 mg/kg; p.o.; daily; 3-5 consecutive months) rescues cognitive deficits, reduces dense-core amyloid plaque load by up to 64%, lowers neuroinflammatory markers, normalizes axonal curvature, and upregulates memory-related gene expression in Tg2576 Alzheimer's disease transgenic mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

New Zealand White (male, 2.8 kg)^[2]
Dosage:

40 mg/kg/day
Administration:

p.o.; daily; 8 days
Result:

Left vascular Cox-1 mRNA levels unchanged relative to placebo.
Reduced Cox-2 mRNA levels.
Reduced Cox-2 protein levels by 39%.

Animal Model:

New Zealand White (male, 2.8 kg)^[2]
Dosage:

40 mg/kg/day
Administration:

p.o.; daily; 8 days
Result:

Reduced platelet deposition on subendothelium-induced primary thrombus (severe stenosis, 1690 s^-1) by 63% relative to placebo.
Reduced platelet deposition on tunica media-induced primary thrombus (severe stenosis, 1690 s^-1) by 53% relative to placebo.

Animal Model:

New Zealand White (male, 2.8 kg)^[2]
Dosage:

10 mg/kg
Administration:

i.v.; single dose
Result:

Reduced platelet deposition on subendothelium-induced primary thrombus (mild stenosis, 212 s^-1) by 66% relative to placebo.
Reduced platelet deposition on tunica media-induced primary thrombus (mild stenosis, 212 s^-1) by 48% relative to placebo.

Animal Model:

Tg2576 (gender-matched; starting treatment at 10 or 13 months of age; overexpressing human mutant APP with KM670/671NL on mixed hybrid C57Bl6j/SJL background)^[5]
Dosage:

30 mg/kg
Administration:

p.o.; daily; 3 or 5 consecutive months
Result:

Achieved significantly more platform crossings in Morris water maze probe trials, and restored contextual fear conditioning freezing levels.
Decreased dense-core (Thioflavin-S-reactive) plaque burden by 47% at 13 months and 64% at 18 months, and reduced total Thioflavin-S-positive plaque counts by 37% at 13 months and 57% at 18 months.
Reduced astrocyte counts in the hippocampal CA1 subfield and entorhinal cortex, decreased microglial counts in the CA1 region at both 13 and 18 months, and lowered brain proinflammatory cytokine levels (IL-1β by 70%; TNF-α by 50%) at 13 months.
Ameliorated axonal curvature near plaques (<50 μm) at 13 months and in both peri-plaque and distal regions (>50 μm) at 18 months, and upregulated hippocampal c-fos and BDNF mRNA expression, restoring BDNF levels to those of non-transgenic controls.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 322-79-2
Appearance Solid
Molecular Weight 248.16
Formula C₁₀H₇F₃O₄
Color White to off-white
SMILES

O=C(O)C1=CC=C(C(F)(F)F)C=C1OC(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (402.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0297 mL

20.1483 mL

40.2966 mL

5 mM

0.8059 mL

4.0297 mL

8.0593 mL

10 mM

0.4030 mL

2.0148 mL

4.0297 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3 mg/mL (12.09 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3 mg/mL (12.09 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3 mg/mL (12.09 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. De Miguel LS, 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):811-817. [Content Brief]

[2]. Duran X, et al. Protective effects of triflusal on secondary thrombus growth and vascular cyclooxygenase-2. J Thromb Haemost. 2008;6(8):1385-1392. [Content Brief]

[3]. Anninos H, et al. Triflusal: an old drug in modern antiplatelet therapy. Review of its action, use, safety and effectiveness. Hellenic J Cardiol. 2009 May-Jun;50(3):199-207. [Content Brief]

[4]. Murdoch D, et al. Triflusal: a review of its use in cerebral infarction and myocardial infarction, and as thromboprophylaxis in atrial fibrillation. Drugs. 2006;66(5):671-692. [Content Brief]

[5]. Coma M, et al. Triflusal reduces dense-core plaque load, associated axonal alterations and inflammatory changes, and rescues cognition in a transgenic mouse model of Alzheimer's disease. Neurobiol Dis. 2010;38(3):482-491. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.0297 mL	20.1483 mL	40.2966 mL	100.7415 mL
	5 mM	0.8059 mL	4.0297 mL	8.0593 mL	20.1483 mL
	10 mM	0.4030 mL	2.0148 mL	4.0297 mL	10.0741 mL
	15 mM	0.2686 mL	1.3432 mL	2.6864 mL	6.7161 mL
	20 mM	0.2015 mL	1.0074 mL	2.0148 mL	5.0371 mL
	25 mM	0.1612 mL	0.8059 mL	1.6119 mL	4.0297 mL
	30 mM	0.1343 mL	0.6716 mL	1.3432 mL	3.3580 mL
	40 mM	0.1007 mL	0.5037 mL	1.0074 mL	2.5185 mL
	50 mM	0.0806 mL	0.4030 mL	0.8059 mL	2.0148 mL
	60 mM	0.0672 mL	0.3358 mL	0.6716 mL	1.6790 mL
	80 mM	0.0504 mL	0.2519 mL	0.5037 mL	1.2593 mL
	100 mM	0.0403 mL	0.2015 mL	0.4030 mL	1.0074 mL

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Triflusal

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All COX Isoforms

All Phosphodiesterase (PDE) Isoforms

All NF-κB Isoforms

All NO Synthase Isoforms

All Prostaglandin Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Triflusal Related Classifications

HY-B0531 Related Classifications