| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| ln Vivo |
Gadopentetate (Gd-DTPA) (tail intravenously; 2 and 5 mmol/kg; single dose) exhibits a pyramidal cycle, TCA cycle, activation, and disruption as part of a systemic activating response. An animal model of how group dynamics are disrupted: rat [1]
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| Animal Protocol |
Animal/Disease Models: Rats[1]
Doses: 2 and 5mmol/kg Route of Administration: tail vein injection, single Experimental Results:Observed urinary and serum metabonomic recovery but the metabolic effects of high-dosed (5mmol/kg) lasted long. Observed hyperlipidemia after Gd-DTPA injection. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Gadopentetate is exclusively eliminated in the urine with 83 ± 14% (mean ± SD) of the dose excreted within 6 hours and 91 ± 13% (mean ± SD) by 24 hours, post-injection. 266 ± 43 mL/kg 1.94 +/- 0.28 mL/min/kg [Normal subjects] Metabolism / Metabolites No detectable biotransformation or decomposition. Biological Half-Life Distribution half life 12 minutes, elimination half 100 minutes |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Amounts of gadolinium excreted into breastmilk after maternal gadopentetate are less than 1% of the amount allowed to be given to infants. In addition, because gadopentetate is poorly absorbed orally, it is not likely to reach the bloodstream of the infant or cause any adverse effects in breastfed infants. Gadopentetate releases more free gadolinium than some other gadolinium-containing contrast agents. Some European guidelines recommend a 24-hour interruption of breastfeeding after a dose, but guidelines developed by North American professional organizations state that breastfeeding need not be disrupted after a nursing mother receives a gadolinium-containing contrast medium. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | |
| Additional Infomation |
A complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid (DTPA see pentetic acid), that is given to enhance the image in cranial and spinal MRIs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p706)
A complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid (DTPA see PENTETIC ACID), that is given to enhance the image in cranial and spinal MRIs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p706) Drug Indication For use with magnetic resonance imaging (MRI) in adults, and pediatric patients (2 years of age and older) to visualize lesions with abnormal vascularity in the brain (intracranial lesions), spine and associated tissues as well as lesions with abnormal vascularity in the head and neck. Also used to facilitate the visualization of lesions with abnormal vascularity in the body (excluding the heart). FDA Label Mechanism of Action Based on the behavior of protons when placed in a strong magnetic field, which is interpreted and transformed into images by magnetic resonance (MR) instruments. MR images are based primarily on proton density and proton relaxation dynamics. MR instruments are sensitive to two different relaxation processes, the T1 (spin-lattice or longitudinal relaxation time) and T2 (spin-spin or transverse relaxation time). Paramagnetic agents contain one or more unpaired electrons that enhance the T1 and T2 relaxation rates of protons in their molecular environment. The proton relaxation effect (PRE) of an unpaired electron is 700 times stronger than that of a proton itself. In MRI, visualization of normal and pathological brain tissue depends in part on variations in the radio frequency signal intensity that occur with changes in proton density, alteration of the T1, and variation in T2. When placed in a magnetic field, gadopentetate dimeglumine shortens the T1 and T2 relaxation times in tissues where it accumulates. In the central nervous system (CNS), gadopentetate dimeglumine enhances visualization of normal tissues that lack a blood-brain barrier, such as the pituitary gland and the meninges. Gadopentetate dimeglumine does not cross the intact blood-brain barrier; therefore, it does not accumulate in normal brain tissue or in CNS lesions that have not caused an abnormal blood-brain barrier (e.g., cysts, mature post-operative scars). Abnormal vascularity or disruption of the blood-brain barrier allows accumulation of gadopentetate dimeglumine in lesions such as neoplasms, abscesses, and subacute infarcts. Outside the CNS, gadopentetate dimeglumine rapidly reaches equilibrium in the interstitial compartment and enhances signal in all tissues as a function of delivery and size of the interstitial compartment. This compound has also been found to inhibit human erythrocyte 6-phosphogluconate dehydrogenase. |
| Molecular Formula |
C14H18GDN3O10.2H
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|---|---|
| Molecular Weight |
547.57
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| Exact Mass |
548.039
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| CAS # |
80529-93-7
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| PubChem CID |
16212436
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| Appearance |
White to off-white solid powder
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| Boiling Point |
721.1ºC at 760 mmHg
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| Melting Point |
129ºC (dec.)(lit.)
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| Flash Point |
389.9ºC
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
29
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| Complexity |
497
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JBUMALASVLVYKI-UHFFFAOYSA-K
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| InChi Code |
InChI=1S/C14H23N3O10.Gd.H2O/c18-10(19)5-15(1-3-16(6-11(20)21)7-12(22)23)2-4-17(8-13(24)25)9-14(26)27;;/h1-9H2,(H,18,19)(H,20,21)(H,22,23)(H,24,25)(H,26,27);;1H2/q;+3;/p-3
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| Chemical Name |
2-[bis[2-[carboxylatomethyl(carboxymethyl)amino]ethyl]amino]acetate;gadolinium(3+);hydrate
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O : ~100 mg/mL (~182.63 mM)
DMSO : ~1 mg/mL (~1.83 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (182.63 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8263 mL | 9.1313 mL | 18.2625 mL | |
| 5 mM | 0.3653 mL | 1.8263 mL | 3.6525 mL | |
| 10 mM | 0.1826 mL | 0.9131 mL | 1.8263 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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