| Size | Price | Stock | Qty |
|---|---|---|---|
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
Purity: =94.45%
| Targets |
3,4,3-LI(1,2-HOPO) targets actinide ions such as plutonium (Pu), americium (Am), uranium (U), neptunium (Np), and curium (Cm). It acts as a metal chelating agent that exhibits a very high affinity for lanthanide and actinide metal ions. By forming stable complexes with these radionuclides, the compound facilitates their excretion from the body, reducing the radiation dose to tissues.
|
|---|---|
| ln Vitro |
In vitro, 3,4,3-LI(1,2-HOPO) is a metal chelating agent that exhibits a very high affinity for lanthanide metal ions. The compound forms highly stable, water-soluble complexes with f-block metal ions. It demonstrates 10-100× greater potency than the currently approved chelator DTPA (diethylenetriaminepentaacetic acid).
|
| ln Vivo |
In vivo, 3,4,3-LI(1,2-HOPO) is being developed as an orally bioavailable, broad-spectrum chelator suitable for mass-casualty deployment. It is effective against Pu, Am, U, Np, and Cm, and has demonstrated prophylactic efficacy 48 hours pre-exposure. It provides 10-fold superior actinide body burden reduction in wound contamination models vs. DTPA at equivalent regimens.
|
| Enzyme Assay |
In vitro assays for 3,4,3-LI(1,2-HOPO) involve measuring its metal chelation properties. The compound's affinity for actinide ions is assessed using competitive binding assays or isothermal titration calorimetry (ITC). Stability constants for the metal-ligand complexes are determined. The compound's ability to remove radionuclides from biological matrices is evaluated in vitro using contaminated cell culture media or protein solutions.
|
| Cell Assay |
Cellular assays for 3,4,3-LI(1,2-HOPO) are performed using cell lines exposed to radionuclides. Cells are treated with the compound, and the intracellular accumulation of radionuclides is measured. The compound's ability to reduce radionuclide uptake and promote efflux from cells is assessed. Cytotoxicity is evaluated using standard viability assays.
|
| Animal Protocol |
In vivo animal studies for 3,4,3-LI(1,2-HOPO) are conducted in rodent models of radionuclide contamination. Animals are exposed to plutonium, americium, or other actinides, and then treated with the compound orally or intravenously. Tissue distribution of radionuclides is measured, and the reduction in body burden is calculated. Wound contamination models are also used.
|
| ADME/Pharmacokinetics |
3,4,3-LI(1,2-HOPO) is an orally bioavailable compound. Its oral formulation enables rapid mass distribution and self-administration, removing IV bottlenecks in emergency response. The compound is soluble in DMSO and should be stored in a dry, dark place at 0-4°C for short-term storage or -20°C for long-term storage.
|
| Toxicity/Toxicokinetics |
3,4,3-LI(1,2-HOPO) has been evaluated for safety in preclinical studies. As a chelating agent, its primary toxicity concern is the potential depletion of essential metal ions (e.g., zinc, copper) from the body. However, the compound is designed to have high selectivity for actinides over essential metals. Specific toxicological data are not detailed in the available sources.
|
| Additional Infomation |
3,4,3-LI(1,2-HOPO) is a preclinical candidate for actinide decorporation. It is being developed as an orally bioavailable, broad-spectrum chelator for treating internal contamination with radionuclides like plutonium and americium. The compound is available from commercial suppliers for research purposes. It is not approved for human use. References describing its development are available.
|
| Molecular Formula |
C34H38N8O12
|
|---|---|
| Molecular Weight |
750.71
|
| Exact Mass |
750.26
|
| CAS # |
110874-36-7
|
| PubChem CID |
132648
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
0.9
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
17
|
| Heavy Atom Count |
54
|
| Complexity |
1690
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KUWKQASGHNTJAT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C34H38N8O12/c43-27-13-3-9-23(39(27)51)31(47)35-17-7-21-37(33(49)25-11-5-15-29(45)41(25)53)19-1-2-20-38(34(50)26-12-6-16-30(46)42(26)54)22-8-18-36-32(48)24-10-4-14-28(44)40(24)52/h3-6,9-16,51-54H,1-2,7-8,17-22H2,(H,35,47)(H,36,48)
|
| Chemical Name |
1-hydroxy-N-[3-[(1-hydroxy-6-oxopyridine-2-carbonyl)-[4-[(1-hydroxy-6-oxopyridine-2-carbonyl)-[3-[(1-hydroxy-6-oxopyridine-2-carbonyl)amino]propyl]amino]butyl]amino]propyl]-6-oxopyridine-2-carboxamide
|
| 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 | 1.3321 mL | 6.6604 mL | 13.3207 mL | |
| 5 mM | 0.2664 mL | 1.3321 mL | 2.6641 mL | |
| 10 mM | 0.1332 mL | 0.6660 mL | 1.3321 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA