| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Indobufen targets the platelet cyclooxygenase (COX) enzyme. It acts as a reversible inhibitor of platelet cyclooxygenase activity. By inhibiting this enzyme, Indobufen suppresses the synthesis of thromboxane A2 (TxA2), which is a key mediator of platelet aggregation and vasoconstriction. This mechanism underlies its antiplatelet and antithrombotic effects.
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| ln Vitro |
Indobufen lowers TxB2 levels but has no effect on the Cox-1 or Cox-2 proteins. In LPS-stimulated monocytes, indomufen suppresses the production of TxA2, but not PGE2. While the amount of phosphorylated p38 remains unchanged, indofufen lowers the degree of ERK1/2 phosphorylation [1].
Indobufen inhibits platelet aggregation in vitro. Its activity is characterized by its ability to reversibly inhibit platelet COX, thereby reducing the production of TxA2. The compound down-regulates tissue factor (TF) in monocytes, further contributing to its antithrombotic effects. Its in vitro activity has been confirmed in various platelet function assays. |
| ln Vivo |
Indobufen possesses anti-coagulant and anti-thrombotic effects in vivo, which can improve micro-inflammatory status and renal function. It has been used in clinical trials for the supportive care and prevention of Atrial Fibrillation. Its ability to inhibit platelet aggregation and suppress thromboxane synthesis contributes to its therapeutic effects in cardiovascular diseases.
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| Enzyme Assay |
The primary in vitro assay for Indobufen involves measuring platelet aggregation in platelet-rich plasma (PRP) using aggregometry. Platelets are pre-incubated with the compound, and aggregation is induced by an agonist such as ADP or collagen. The inhibition of aggregation is measured to determine the compound's potency. Additionally, the inhibition of COX activity can be assessed by measuring the production of TxA2.
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| Cell Assay |
Cellular assays for Indobufen involve treating platelets or monocytes with the compound and measuring its effects. In platelets, the inhibition of TxA2 synthesis and platelet aggregation can be assessed. In monocytes, the down-regulation of tissue factor (TF) expression can be measured. These assays confirm the compound's antiplatelet and anti-inflammatory activities at the cellular level.
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| Animal Protocol |
In vivo animal experiments for Indobufen would typically involve administering the compound to animal models of thrombosis or inflammation to assess its antithrombotic and anti-inflammatory effects. Parameters such as platelet aggregation, thrombus formation, and inflammatory markers would be measured. However, specific in vivo data is not detailed in the provided sources.
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| ADME/Pharmacokinetics |
Indobufen has a molecular weight of 295.3 g/mol and a molecular formula of C18H17NO3. It has an XLogP3 value of 3.1. The compound is a member of isoindoles. Its pharmacokinetic properties, such as oral bioavailability and half-life, would have been characterized during its clinical development.
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| Toxicity/Toxicokinetics |
The toxicological profile of Indobufen is characteristic of antiplatelet agents. Common adverse effects may include bleeding, gastrointestinal disturbances, and allergic reactions. Its safety has been evaluated in clinical trials for the prevention of Atrial Fibrillation. As a reversible COX inhibitor, its effects are generally reversible upon discontinuation.
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| References | |
| Additional Infomation |
Indobufen belongs to the isoindole class of compounds. Indobufen has been used in trials investigating supportive care and prevention of atrial fibrillation. See also: Indobufen, (S)- (Note moved to).
Indobufen is an antiplatelet agent that has been investigated for the prevention of Atrial Fibrillation. It is a reversible inhibitor of platelet cyclooxygenase, which distinguishes it from irreversible COX inhibitors like aspirin. The compound is also known as Ibustrin and K 3920. It is available for research purposes from various chemical suppliers. |
| Molecular Formula |
C18H17NO3
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|---|---|
| Molecular Weight |
295.3325
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| Exact Mass |
295.12
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| CAS # |
63610-08-2
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| Related CAS # |
Indobufen-d5
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| PubChem CID |
107641
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
518.1±50.0 °C at 760 mmHg
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| Melting Point |
33-34 °C(lit.)
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| Flash Point |
267.1±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.630
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
428
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AYDXAULLCROVIT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17NO3/c1-2-15(18(21)22)12-7-9-14(10-8-12)19-11-13-5-3-4-6-16(13)17(19)20/h3-10,15H,2,11H2,1H3,(H,21,22)
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| Chemical Name |
2-[4-(3-oxo-1H-isoindol-2-yl)phenyl]butanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~846.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3860 mL | 16.9302 mL | 33.8604 mL | |
| 5 mM | 0.6772 mL | 3.3860 mL | 6.7721 mL | |
| 10 mM | 0.3386 mL | 1.6930 mL | 3.3860 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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