| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
When administered ioxitalamate is not absorbed in the GI tract. In the case of presence of an intestinal perforation, ioxitalamate is completely absorbed. When administered intravascularly, ioxitalamate is rapidly distributed in the interstitial space and intravascular compartment. As ioxitalamate is not absorbed in the normal intestine, the elimination route of this compound is entirely performed by the feces. When absorbed due to the presence of an intestinal perforation, ioxitalamate presents a rapid renal elimination. when ioxitalamate is administered intravascularly, it is eliminated unchanged mainly via renal excretion through glomerular filtration without reabsorption or tubular secretion. In the cases of renal failure, the elimination is mainly performed in the biliary, salivary, sudoral and colic route. The volume of distribution of ioxitalamate is 194 ml/kg. The total clearance rate of ioxitalamate is 120 ml/min. Metabolism / Metabolites The rapid clearance suggests that ioxitalamate is not metabolized in the body. Biological Half-Life The elimination half-life of ioxitalamate is 1.1 hours. |
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| Toxicity/Toxicokinetics |
Protein Binding
Iodinated monomeric contrast agents are rarely bound to plasma proteins and when they bind, usually the association is very weak. When bound, it only represents from 0 to 27% of the ioxitalamate administered dose. |
| References | |
| Additional Infomation |
Iooxitalamic acid is an organoiodine compound that is 2,4,6-triiodobenzoic acid substituted by an acetylamino group at position 3 and a (2-hydroxyethyl)carbamoyl group at position 5. It is used as a contrast medium. It has a role as a xenobiotic, an environmental contaminant and a radioopaque medium. It is a dicarboxylic acid monoamide, a member of acetamides, an organoiodine compound and a member of benzoic acids.
Ioxitalamate is an ionic iodinated contrast medium. It is a first-generation contrast media formed by an ionic monomer with a high osmolarity of 1500-1800 mOsm/kg. Ioxitalamic acid in the salt forms of sodium and meglumine was developed by Liebel-Flarshem Canada Inc and approved by Health Canada in 1995. Until the last review in 2015, this drug is still available in the market. Drug Indication Ioxitalamate in both of its available forms is indicated for exploration of the digestive tract by tomodensitometry or by regular gastroduodenal radiography. Its use is restrained to the cases in which the administration of barium sulfate is not recommended or contraindicated. The intravascular administration of ioxitalamate is contraindicated as it may present significant side effects. Mechanism of Action Ioxitalamate acts as a bowel opacifier which facilitates the interpretation of the anatomy and differentiation of bowel loops from soft tissue masses. Pharmacodynamics Ioxitalamate presents a very large osmolality which is related to the presence of renal toxicity, vasodilatation, bradycardia and pulmonary hypertension. This large osmolality allows ioxitalamate to move slowly in the bowel allowing for analysis for later follow excretion in the feces. |
| Molecular Formula |
C12H11I3N2O5
|
|---|---|
| Molecular Weight |
643.94
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| Exact Mass |
643.78
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| CAS # |
28179-44-4
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| Related CAS # |
33954-26-6 (hydrochloride salt);29288-99-1 (meglumine ioxithalamate salt/solvate)
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| PubChem CID |
34536
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| Appearance |
Typically exists as solid at room temperature
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| Density |
2.519g/cm3
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| Boiling Point |
582.8ºC at 760mmHg
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| Melting Point |
253-255?C
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| Flash Point |
306.3ºC
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| Vapour Pressure |
1.99E-14mmHg at 25°C
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| LogP |
2.343
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
451
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(O)C1=C(I)C(C(NCCO)=O)=C(I)C(NC(C)=O)=C1I
|
| InChi Key |
OLAOYPRJVHUHCF-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
3-acetamido-5-(2-hydroxyethylcarbamoyl)-2,4,6-triiodobenzoic acid
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| Synonyms |
Vasobrix; Telebrix; Ioxitalamic 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) |
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
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|---|---|
| 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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