| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Picotamide targets thromboxane A2 (TxA2) synthase and the thromboxane A2 receptor. As a combined inhibitor, it both reduces the production of TxA2 and blocks its action at the receptor. The compound has a Kd of 325 nM for the TxA2 receptor. This dual mechanism contributes to its antiplatelet and antithrombotic effects.
|
|---|---|
| ln Vitro |
In vitro, Picotamide is a thromboxane A2 (TXA2) receptor antagonist and a TXA2 synthase inhibitor. It inhibits platelet aggregation and can inhibit smooth muscle contraction. It shows anticoagulant and fibrinolytic properties. These activities contribute to its antiplatelet effects and potential cardiovascular benefits.
|
| ln Vivo |
In vivo, Picotamide has been shown to protect mice from death in a pulmonary embolism model. In clinical studies, it has been considered as a platelet aggregation inhibitor and has been shown to improve renal function. It promotes the reduction of microalbuminuria and inhibition of carotid plaque growth in diabetes.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Picotamide involve studying its binding to the thromboxane A2 receptor using radioligand binding assays. Thromboxane A2 synthase activity can be measured by quantifying the production of TxA2 or its metabolites in the presence of the compound. Platelet aggregation assays are used to confirm its functional antiplatelet activity.
|
| Cell Assay |
In vitro cellular assays for Picotamide are performed using platelets to assess its anti-aggregatory effects. Platelet-rich plasma is incubated with the compound and then stimulated with aggregating agents such as arachidonic acid or collagen. Platelet aggregation is measured using a platelet aggregometer. Smooth muscle cells can be used to study the inhibition of contraction.
|
| Animal Protocol |
In vivo animal studies with Picotamide have been conducted in a mouse pulmonary embolism model. The compound is administered, and its protective effect against mortality is assessed. Other animal models of thrombosis and diabetes are also used to study its effects on platelet aggregation, microalbuminuria, and carotid plaque growth.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Picotamide are not extensively detailed in the available literature. It is an antiplatelet drug that has been used in clinical studies. Specific parameters such as oral bioavailability, half-life, and metabolism are not detailed in the provided sources.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Picotamide is not extensively detailed in the available literature. As a drug that has been studied clinically, its safety profile would have been evaluated. However, specific toxicity data are not provided in the search results.
|
| References | |
| Additional Infomation |
4-Methoxy-N1,N3-bis(3-pyridylmethyl)benzene-1,3-dicarboxamide is a member of the benzamide class of compounds.
Picotamide is a combined inhibitor of thromboxane A2 synthase and a receptor antagonist. It has antiplatelet and antithrombotic properties and has shown benefits in reducing microalbuminuria and carotid plaque growth in diabetes. It is used in cardiovascular research and is available for research purposes. |
| Molecular Formula |
C21H20N4O3
|
|---|---|
| Molecular Weight |
376.4085
|
| Exact Mass |
376.154
|
| CAS # |
32828-81-2
|
| Related CAS # |
Picotamide monohydrate; 80530-63-8
|
| PubChem CID |
4814
|
| Appearance |
White to off-white solid powder
|
| Density |
1.246g/cm3
|
| Boiling Point |
668.1ºC at 760mmHg
|
| Melting Point |
124ºC
|
| Flash Point |
357.8ºC
|
| Index of Refraction |
1.614
|
| LogP |
3.127
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
28
|
| Complexity |
516
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=CC=C(OC)C(C(NCC2=CC=CN=C2)=O)=C1)NCC3=CC=CN=C3
|
| InChi Key |
KYWCWBXGRWWINE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H20N4O3/c1-28-19-7-6-17(20(26)24-13-15-4-2-8-22-11-15)10-18(19)21(27)25-14-16-5-3-9-23-12-16/h2-12H,13-14H2,1H3,(H,24,26)(H,25,27)
|
| Chemical Name |
4-methoxy-1-N,3-N-bis(pyridin-3-ylmethyl)benzene-1,3-dicarboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~5 mg/mL (~13.3 mM; with ultrasonication and warming)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% 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 DMSO stock solution (5.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.33 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 DMSO stock solution (5.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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 3: ≥ 0.5 mg/mL (1.33 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 DMSO stock solution (5.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6567 mL | 13.2834 mL | 26.5668 mL | |
| 5 mM | 0.5313 mL | 2.6567 mL | 5.3134 mL | |
| 10 mM | 0.2657 mL | 1.3283 mL | 2.6567 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
