| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Iocitalazine is not absorbed in the gastrointestinal tract. In the presence of intestinal perforation, iocitalazine is completely absorbed. When administered intravenously, iocitalazine is rapidly distributed in the interstitial space and intravascular space. Since iocitalazine is not absorbed in the normal intestine, it is excreted entirely via feces. If absorbed due to intestinal perforation, iocitalazine is rapidly excreted by the kidneys. When administered intravenously, iocitalazine is primarily excreted unchanged via glomerular filtration, without reabsorption or tubular secretion. In renal failure, iocitalazine is primarily cleared via bile, saliva, sweat glands, and the colon. The volume of distribution of iocitalazine is 194 ml/kg. The total clearance of iocitalazine is 120 ml/min. Metabolism/Metabolites Rapid clearance indicates that iocitalazine is not metabolized in the body. Biological Half-Life The elimination half-life of iodocitalac is 1.1 hours. |
|---|---|
| Toxicity/Toxicokinetics |
Protein Binding
Iodinated monomeric contrast agents rarely bind to plasma proteins, and even when they do, the binding affinity is usually very weak. After binding, they account for only 0% to 27% of the administered iodine dose. |
| References | |
| Additional Infomation |
Iooxitalamic is an organic iodine compound composed of 2,4,6-triiodobenzoic acid with an acetamino group at the 3-position and a (2-hydroxyethyl)carbamoyl group at the 5-position. It is used as a contrast agent. It is both an exogenous substance and an environmental pollutant and a radioactive opacifier. It is a dicarboxylic acid monoamide, belonging to the acetamide class, organic iodine compounds, and benzoic acid compounds. Iooxitalamic is an ionic iodinated contrast agent. It is a first-generation contrast agent, composed of ionic monomers with high osmotic pressure (1500-1800 mOsm/kg). Sodium Iooxitalamic and Iooxitalamic meglumine were developed by Liebel-Flarshem Canada Inc. and approved by Health Canada in 1995. As of the most recent review in 2015, the drug was still marketed.
Drug Indications Both iocitalazine sodium and iocitalazine meglumine salt are indicated for exploration of the digestive tract via CT scan or routine gastroduodenal X-ray. Their use is limited to situations where barium sulfate is not recommended or contraindicated. Intravenous administration of iocitalazine is contraindicated due to its potential to cause serious side effects.Mechanism of Action Iocitalazine is an intestinal contrast agent that aids in the visualization of anatomical structures and the differentiation of intestinal loops from soft tissue masses.Pharmacodynamics Iocitalazine has an extremely high osmolarity, which is associated with nephrotoxicity, vasodilation, bradycardia, and pulmonary hypertension. This high osmolarity causes iocitalazine to move slowly through the intestines, facilitating subsequent analysis of its excretion in feces. |
| Molecular Formula |
C12H11I3N2O5
|
|---|---|
| Molecular Weight |
643.94
|
| Exact Mass |
643.78
|
| CAS # |
28179-44-4
|
| Related CAS # |
33954-26-6 (hydrochloride salt);29288-99-1 (meglumine ioxithalamate salt/solvate)
|
| PubChem CID |
34536
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
2.519g/cm3
|
| Boiling Point |
582.8ºC at 760mmHg
|
| Melting Point |
253-255?C
|
| Flash Point |
306.3ºC
|
| Vapour Pressure |
1.99E-14mmHg at 25°C
|
| LogP |
2.343
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
22
|
| Complexity |
451
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(O)C1=C(I)C(C(NCCO)=O)=C(I)C(NC(C)=O)=C1I
|
| InChi Key |
OLAOYPRJVHUHCF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H11I3N2O5/c1-4(19)17-10-8(14)5(11(20)16-2-3-18)7(13)6(9(10)15)12(21)22/h18H,2-3H2,1H3,(H,16,20)(H,17,19)(H,21,22)
|
| Chemical Name |
3-acetamido-5-(2-hydroxyethylcarbamoyl)-2,4,6-triiodobenzoic acid
|
| Synonyms |
Vasobrix; Telebrix; Ioxitalamic Acid
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5529 mL | 7.7647 mL | 15.5294 mL | |
| 5 mM | 0.3106 mL | 1.5529 mL | 3.1059 mL | |
| 10 mM | 0.1553 mL | 0.7765 mL | 1.5529 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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