| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
Diagnostic tool for AD (Alzheimer's disease)
AV-105 is a precursor compound used in the synthesis of radiolabeled imaging agents. It is not a drug with a direct biological target but is a chemical intermediate for the production of Florbetapir (18F), which targets amyloid-β (Aβ) plaques in the brain. By enabling the synthesis of this PET imaging agent, AV-105 facilitates the diagnosis of Alzheimer's disease and other neurodegenerative conditions. |
|---|---|
| ln Vitro |
Primary tosylate is used in the AV-105 synthesis process in place of the primary mesylate active leaving group. Since the tosylate formed during the free radical reaction is easily recovered from the 18F-labeled product by chromatography, the use of tosylate precursors for radioactivity is advantageous, at least during the radioactive process [1].
In vitro, AV-105 is used as a precursor in radiochemical synthesis. The AV-105 synthesis method utilizes a primary tosylate instead of a primary mesylate as an active leaving group. Use of the tosylate precursor for radiofluorination is beneficial for the production of ¹⁸F-labeled compounds. It is not typically evaluated for direct biological activity in cell-based assays. |
| ln Vivo |
AV-105 is not typically evaluated for in vivo activity as a standalone compound. Its role is in the synthesis of Florbetapir (18F), which is then used for PET imaging in vivo. Florbetapir (18F) is a PET scanning radiopharmaceutical agent used for imaging of neurodegenerative diseases of the brain such as Alzheimer's disease.
|
| Enzyme Assay |
AV-105 is a chemical reagent, and its purity and identity are confirmed using analytical techniques such as NMR and HPLC. It is not typically used in enzyme or receptor binding assays. Its reactivity as a precursor for radiofluorination can be assessed by reacting it with ¹⁸F-fluoride and monitoring the formation of the radiolabeled product.
|
| Cell Assay |
AV-105 is not typically used in cell-based assays as a standalone compound. Its primary application is in the synthesis of Florbetapir (18F), which is then used in PET imaging studies. The radiolabeled product's binding to Aβ plaques can be assessed in cell-based or tissue-based assays.
|
| Animal Protocol |
AV-105 is not typically used in in vivo animal studies as a standalone compound. It is used to synthesize Florbetapir (18F), which is then administered to animals or humans for PET imaging. The imaging agent's biodistribution and binding to Aβ plaques are assessed in vivo.
|
| ADME/Pharmacokinetics |
AV-105 has a molecular formula of C₃₂H₄₀N₂O₈S and a molecular weight of 612.73 g/mol. Its CAS number is 1205550-99-7. The purity is typically ≥95%. It is a small molecule precursor for radiolabeled compound synthesis. It should be stored according to the manufacturer's instructions.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for AV-105 are not extensively detailed in the available literature. As a chemical precursor used in the synthesis of imaging agents, its toxicity is typically assessed as part of the final radiolabeled product. Standard safety precautions should be taken when handling AV-105 in the laboratory.
|
| References |
[1]. Tyler Benedum, et al. Synthesis of 18f-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof. WO2010078370A1.
|
| Additional Infomation |
randomized, multicenter, multinational study aimed to evaluate flubetapirid (18F) PET in participants enrolled in the IRCSFBF protocol. EudraCT: 2012-002595-13 Phase: Phase 3 Status: Completed Date: March 1, 2013
AV-105 is a precursor for the synthesis of Florbetapir (18F) (Amyvid), a PET imaging agent targeting Aβ plaques for the diagnosis of Alzheimer's disease. It is a chemical intermediate used in radiopharmaceutical research and development. AV-105 is not a therapeutic agent but a valuable tool for the production of diagnostic imaging agents. |
| Molecular Formula |
C27H32N2O6S
|
|---|---|
| Molecular Weight |
612.73360824585
|
| Exact Mass |
612.251
|
| Elemental Analysis |
C, 63.26; H, 6.29; N, 5.46; O, 18.73; S, 6.25
|
| CAS # |
1205550-99-7
|
| PubChem CID |
46842948
|
| Appearance |
White to off-white solid powder
|
| LogP |
6.83
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
17
|
| Heavy Atom Count |
43
|
| Complexity |
932
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C1C=CC(C)=CC=1)(=O)(=O)OCCOCCOCCOC1C=CC(=CN=1)/C=C/C1C=CC(=CC=1)N(C)C(=O)OC(C)(C)C
|
| InChi Key |
CDONYNLHUQSRJH-AATRIKPKSA-N
|
| InChi Code |
InChI=1S/C27H32N2O6S/c1-22-3-12-26(13-4-22)36(30,31)35-20-18-33-16-15-32-17-19-34-27-14-9-24(21-29-27)6-5-23-7-10-25(28-2)11-8-23/h3-14,21,28H,15-20H2,1-2H3/b6-5+
|
| Chemical Name |
(E)-4-(2-(6-(2-(2-(2-Tosyloxyethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)-N-methyl benzenamine
|
| Synonyms |
AV-105; AV 105; AV105.
|
| 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) |
DMSO : ~62.5 mg/mL (~102.00 mM)
|
|---|---|
| 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 | 1.6320 mL | 8.1602 mL | 16.3204 mL | |
| 5 mM | 0.3264 mL | 1.6320 mL | 3.2641 mL | |
| 10 mM | 0.1632 mL | 0.8160 mL | 1.6320 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