| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
Cyclo-oxygenase (COX-1 and COX-2), the enzymes responsible for the conversion of arachidonic acid to prostaglandins and thromboxanes. Carbasalate calcium is a non-selective cyclo-oxygenase inhibitor. The antithrombotic effect is due to the irreversible acetylating of the enzyme cyclo-oxygenase in the thrombocyte, through which the formation of the prostaglandin thromboxane A2 is inhibited.
|
|---|---|
| ln Vitro |
Carbasalate calcium acts as a non-selective cyclo-oxygenase inhibitor, irreversibly acetylating COX-1 and COX-2 enzymes. This acetylation blocks the conversion of arachidonic acid to prostaglandins and thromboxanes, resulting in analgesic, antipyretic, and anti-inflammatory effects. The antithrombotic effect is due to the irreversible acetylating of cyclo-oxygenase in the thrombocyte, inhibiting the formation of thromboxane A2. Carbasalate calcium reduces carrageenan-induced paw edema in rats.
|
| ln Vivo |
In vivo, carbasalate calcium has analgesic, antipyretic, anti-inflammatory, and antiplatelet effects. It reduces carrageenan-induced paw edema in rats. Oral absorption is rapid with a fast onset of action and high bioavailability. The compound's antipyretic and analgesic effects are stronger than aspirin, with fewer adverse reactions. The antithrombotic effect is due to irreversible acetylation of cyclo-oxygenase in platelets, inhibiting thromboxane A2 formation.
|
| Enzyme Assay |
In vitro enzyme assays for carbasalate calcium involve measuring COX-1 and COX-2 inhibition. The enzymes are incubated with arachidonic acid substrate and various concentrations of carbasalate calcium (or its active metabolite salicylate), and the production of prostaglandins is measured by ELISA or other methods. IC50 values are determined from concentration-response curves. These assays confirm the non-selective COX inhibition by carbasalate calcium.
|
| Cell Assay |
Cellular assays for carbasalate calcium involve treating cells (such as platelets or inflammatory cells) with the compound and measuring prostaglandin production or platelet aggregation. The compound's ability to inhibit thromboxane A2 formation and platelet aggregation is demonstrated in these assays. These assays confirm the antiplatelet and anti-inflammatory effects of carbasalate calcium.
|
| Animal Protocol |
In vivo animal studies for carbasalate calcium typically involve administration to rodent models of inflammation or pain. The compound reduces carrageenan-induced paw edema in rats. Other models include the acetic acid-induced writhing test for analgesia and the yeast-induced fever model for antipyretic effects. These studies establish the analgesic, anti-inflammatory, and antipyretic efficacy of carbasalate calcium.
|
| ADME/Pharmacokinetics |
Pharmacokinetic studies show that carbasalate calcium is rapidly absorbed after oral administration with a fast onset of action and high bioavailability. Its antipyretic and analgesic effects are stronger than aspirin, with fewer adverse reactions. Following absorption, carbasalate calcium is hydrolyzed to acetylsalicylic acid (aspirin) and salicylic acid, which are responsible for its pharmacological effects. The compound is freely soluble in water.
|
| Toxicity/Toxicokinetics |
The adverse effects of carbasalate calcium are dose-dependent and due to the pharmacological effect of acetylsalicylic acid. Common adverse effects include gastrointestinal irritation, nausea, vomiting, and increased risk of bleeding due to its antiplatelet effect. The compound is contraindicated in patients with active peptic ulcer disease, severe bleeding disorders, or aspirin allergy. On the basis of the pharmacodynamic profile and/or adverse reactions profile, it is unlikely that carbasalate calcium affects the ability to drive and use machines.
|
| References | |
| Additional Infomation |
See other relationships...
Carbasalate calcium is a calcium-urea chelate of aspirin (acetylsalicylic acid) with analgesic, anti-inflammatory, antipyretic, and antiplatelet effects. It is a non-selective cyclo-oxygenase inhibitor. Oral absorption is rapid with fast onset of action and high bioavailability, and its antipyretic and analgesic effects are stronger than aspirin with fewer adverse reactions. The antithrombotic effect is due to irreversible acetylation of cyclo-oxygenase in platelets, inhibiting thromboxane A2 formation. |
| Molecular Formula |
C19H18CAN2O9
|
|---|---|
| Molecular Weight |
458.436
|
| Exact Mass |
458.063
|
| CAS # |
5749-67-7
|
| Related CAS # |
52080-78-1 (Parent);50-78-2 (Parent)
|
| PubChem CID |
21975
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
321.4ºC at 760 mmHg
|
| Flash Point |
131.2ºC
|
| LogP |
2.89
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
31
|
| Complexity |
235
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(=O)OC1=CC=CC=C1C(=O)[O-].CC(=O)OC1=CC=CC=C1C(=O)[O-].C(=O)(N)N.[Ca+2]
|
| InChi Key |
VYMUGTALCSPLDM-UHFFFAOYSA-L
|
| InChi Code |
InChI=1S/2C9H8O4.CH4N2O.Ca/c2*1-6(10)13-8-5-3-2-4-7(8)9(11)12;2-1(3)4;/h2*2-5H,1H3,(H,11,12);(H4,2,3,4);/q;;;+2/p-2
|
| Chemical Name |
calcium;2-acetyloxybenzoate;urea
|
| Synonyms |
Alcacyl; Iromin; Carbasalate Calcium
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~385.74 mM)
DMSO : ~5 mg/mL (~19.29 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 (1.93 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 5.0 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. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1813 mL | 10.9066 mL | 21.8131 mL | |
| 5 mM | 0.4363 mL | 2.1813 mL | 4.3626 mL | |
| 10 mM | 0.2181 mL | 1.0907 mL | 2.1813 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02565693
Conditions:Cerebral Hemorrhage|Atrial FibrillationProducts are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
