| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
After intravenous administration, acetrizoic acid gets largely distributed in the extracellular fluid space. Radiographic agents like acetrizoic agents present variations in the plasma concentration depending on the dose and injection rate. After 5 minutes of administration, about 80% of the administered dose will stay outside of the intravascular compartment. There are some exceptions to the diffusion, such as the brain, neural tissue and testes where the tight junctions do not allow extravascularization. After intravenous administration, acetrizoic acid is mainly excreted unchanged by the kidney. The elimination pathway is handled by a glomerular filtration and concentration by tubular resorption of water. The excreted dose is of about 83% of the administered dose after 3 hours and of about 100% at 24 hours. Metabolism / Metabolites The majority of the administered dose of acetrizoic acid remains unchanged. Biological Half-Life When water-soluble contrast agents, such as acetrizoic acid, are administered, it is reported a half-life of approximate 4 hours. |
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| Toxicity/Toxicokinetics |
Protein Binding
The radiographic agents such as acetrizoic acid are carried free in plasma in which less than 5% of the injected dose is protein bound. |
| References |
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| Additional Infomation |
Acetrizoic acid is an aminobenzoic acid.
Acetrizoic acid presents the molecular formula of 3-acetamidol-2,4,6-triiodobenzoic acid and it is the first monomeric ionic compound used as an X-ray contrast agent. It was first synthesized by Wallingford in 1953 and it was filled in the FDA by the Johnson & Johnson subsidiary, Cilag Chemie AG, on February 8th, 1978. Acetrizoic acid presents, in the FDA records, a category of drug substance with an inactive status. An iodinated radiographic contrast medium used as acetrizoate sodium in HYSTEROSALPINGOGRAPHY. Drug Indication Acetrizoic acid indication was to be used as a contrast agent for X-ray. Some information indicates its nephrotropic property as one of the characteristics for the utilization of acetrizoic acid. The X-ray imaging depends on the difference in tissue density which is provided by an X-ray attenuation between the area of interest and the surrounding tissue. The use of contrast agents will provoke a contrast enhancement or opacification and it will improve the differentiation of pathological processes from normal tissue. Mechanism of Action Iodine, a big component in acetrizoic acid, is an element with a high atomic density. This property causes attenuation of X-rays within the diagnostic energy spectrum. Thus, acetrizoic acid is a water-soluble and reasonably safe iodinated contrast agent that can be intravenously administered for clinical applications. |
| Molecular Formula |
C9H6I3NO3
|
|---|---|
| Molecular Weight |
556.8623
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| Exact Mass |
556.748
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| CAS # |
85-36-9
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| PubChem CID |
6806
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| Appearance |
White to off-white solid powder
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| Density |
2.8±0.1 g/cm3
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| Boiling Point |
547.1±50.0 °C at 760 mmHg
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| Flash Point |
284.7±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.802
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| LogP |
1.04
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
300
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
IC1=C(C(=O)O[H])C(=C([H])C(=C1N([H])C(C([H])([H])[H])=O)I)I
|
| InChi Key |
GNOGSFBXBWBTIG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H6I3NO3/c1-3(14)13-8-5(11)2-4(10)6(7(8)12)9(15)16/h2H,1H3,(H,13,14)(H,15,16)
|
| Chemical Name |
3-acetamido-2,4,6-triiodobenzoic 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 : ≥ 5.6 mg/mL (~10.06 mM)
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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 | 1.7958 mL | 8.9789 mL | 17.9578 mL | |
| 5 mM | 0.3592 mL | 1.7958 mL | 3.5916 mL | |
| 10 mM | 0.1796 mL | 0.8979 mL | 1.7958 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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