| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg | |||
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| Targets |
Butyrylcholinesterase (BuChE). TRV-7019 is a radioligand, meaning it binds to its target (BuChE) with high affinity and selectivity. Butyrylcholinesterase is an enzyme that, like AChE, hydrolyzes choline-based esters. In the healthy brain, BuChE activity is low, but its levels are significantly elevated in the brains of patients with Alzheimer's disease, multiple sclerosis, and certain brain tumors. It is a promising biomarker for these conditions. The ability to cross the BBB (blood-brain barrier) is a critical design feature.
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| ln Vitro |
No specific in vitro activity data has been reported. As a radioligand, its potency is defined by its binding affinity (Ki or Kd) and selectivity for BuChE over other cholinesterases (like AChE). The radioligand is designed to be a potent and selective BuChE inhibitor with minimal off-target binding. The presence of the radiolabel (e.g., 11C or 18F) allows for its detection by PET (positron emission tomography). The compound is evaluated for its binding capacity in brain homogenates.
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| ln Vivo |
TRV-7019 is a BBB-penetrable radioligand for brain imaging that targets butyrylcholinesterase. It is used for the diagnosis of an amyloid disease, multiple sclerosis, a brain tumor, or butyrylcholinesterase activity. The compound is not used for therapeutic purposes but as an imaging agent to visualize BuChE distribution and activity in the living brain.
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| Enzyme Assay |
TRV-7019 is a BBB-penetrable radioligand that targets butyrylcholinesterase. For a cell-free binding assay, a typical protocol involves using a membrane preparation of BuChE (e.g., from human serum or recombinant). Various concentrations of unlabeled TRV-7019 are incubated with a fixed, low concentration of a radiolabeled high-affinity BuChE tracer (e.g., 3H-labeled) in Tris-HCl buffer (pH 7.4) at 25degC for 60-90 minutes. The reaction is terminated by rapid filtration through a glass fiber filter, and the bound radioactivity is counted. Non-specific binding is determined in the presence of a saturating concentration of a known BuChE inhibitor. The half-maximal inhibitory concentration (IC50) is calculated, and the inhibition constant (Ki) is derived using the Cheng-Prusoff equation.
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| Cell Assay |
For cell-based assays, the target is the BuChE protein, not a cell type. However, to study cell uptake and binding, a BuChE-overexpressing cell line (e.g., HEK293 cells transfected with the BCHE gene) or human neuroblastoma cells (SH-SY5Y, which express BuChE) are used. Cells are seeded in 24-well plates and grown to confluence. The radiolabeled TRV-7019 (or a fluorescent derivative) is added to the cells at concentrations of 0.1-100 nM, with or without excess unlabeled TRV-7019 to block specific binding. After 1-2 hours of incubation at 37degC, cells are washed to remove unbound compound, and the cell-associated radioactivity is measured in a gamma counter (for PET isotopes) or fluorescence is read in a plate reader. This experiment determines the specificity of the radioligand for BuChE on intact cells.
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| Animal Protocol |
For an in vivo PET imaging study, a typical protocol would involve intravenous (i.v.) injection of the radiolabeled TRV-7019 (e.g., 5-15 mCi, 200 uL) into the tail vein of 8-12 week old mice, rats, or non-human primates. The animal models could include wild-type animals for baseline, or animal models of Alzheimer's (e.g., APP/PS1 transgenic mice) or a glioma model (e.g., GL261 or U87 cells implanted orthotopically). Dynamic PET/CT (or PET/MR) scans are acquired over 60-90 minutes. Regions of interest (ROIs) in the brain are drawn, and time-activity curves (TACs) are generated to calculate the standard uptake value (SUV) and the distribution volume (VT). The specificity of the tracer is confirmed by a blocking study, where a non-radioactive BuChE inhibitor is co-injected to block the signal.
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| ADME/Pharmacokinetics |
TRV-7019 is designed to be a BBB-penetrable radioligand. For a PET tracer, the pharmacokinetic profile is critical. It must rapidly cross the BBB after i.v. injection, achieve a high peak brain uptake (Cmax), and then wash out from non-specific binding regions. The clearance is typically fast, allowing for imaging within 60-90 minutes post-injection. The compound's half-life (t½) in the brain must be matched to the half-life of the positron-emitting isotope (e.g., 68Ga ~68 min, 18F ~110 min, 11C ~20 min). The tracer must have high in vivo stability to prevent radioactive metabolites from entering the brain and confounding the signal. The logP (lipophilicity) of the compound is optimized (usually ~2-3) to ensure BBB penetration.
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| Toxicity/Toxicokinetics |
No specific toxicity data has been reported for the unlabeled compound. For a PET radioligand, the tracer is typically administered in sub-pharmacological doses (a "microdose," usually < 1-10 ug for a human scan), so the chemical toxicity is negligible. The primary risk comes from the radiation exposure from the radioactive isotope, which is low and acceptable for diagnostic procedures (effective dose typically < 10 mSv). For animals, the injected mass must be kept low enough to avoid pharmacological effects (e.g., BuChE inhibition). Safety is confirmed by measuring vital signs and performing blood chemistry before and after the scan. The compound is for research use only.
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| References |
Sultan Darvesh, et al. Butyrylcholinesterase compounds and use in diseases of the nervous system. Patent WO2021026429A1.
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| Additional Infomation |
TRV-7019 is a research radioligand for the molecular imaging of butyrylcholinesterase (BuChE) in the brain. BuChE is considered a biomarker for neuroinflammation, neurodegeneration, and the progression of Alzheimer's disease. It may also have utility in diagnosing and monitoring multiple sclerosis and gliomas. This compound is a valuable tool for understanding the role of BuChE in these conditions. The compound is not approved for clinical diagnostic use; it is a preclinical imaging agent. The specific chemical structure is not provided in the search results, but the isotope to be used is likely either 18F or 11C. IUPAC name and molecular weight were not provided.
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| Molecular Formula |
C14H12INO3
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| Molecular Weight |
369.159
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| Exact Mass |
368.99
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| Elemental Analysis |
C, 45.55; H, 3.28; I, 34.38; N, 3.79; O, 13.00
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| CAS # |
2598164-15-7
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| Appearance |
White to off-white solid powder
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| InChi Key |
AVKHPDWARYICID-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H12INO3/c1-18-13-4-2-3-12(16-13)14(17)19-9-10-5-7-11(15)8-6-10/h2-8H,9H2,1H3
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| Chemical Name |
4-iodobenzyl 6-methoxypicolinate
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| Synonyms |
TRV-7019; TRV 7019; TRV7019;
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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 : ~100 mg/mL (~270.89 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 | 2.7089 mL | 13.5443 mL | 27.0885 mL | |
| 5 mM | 0.5418 mL | 2.7089 mL | 5.4177 mL | |
| 10 mM | 0.2709 mL | 1.3544 mL | 2.7089 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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