| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Paliroden does not have a single defined molecular target. It is an orally active neurotrophic, non-peptidic compound that activates the synthesis of endogenous neurotrophins. Neurotrophins are a family of proteins that promote the survival, growth, and differentiation of neurons. Key neurotrophins include nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), neurotrophin-3 (NT-3), and neurotrophin-4/5 (NT-4/5). By stimulating the synthesis of these endogenous neurotrophins, Paliroden supports neuronal function and survival. The compound's mechanism of action may involve modulation of signaling pathways that regulate neurotrophin expression. Paliroden is indicated for use in Alzheimer's disease and Parkinson's disease research, where neurotrophin levels are often reduced and neuronal survival is compromised. The compound has been investigated in clinical trials for these indications.
|
|---|---|
| ln Vitro |
Paliroden is an orally active neurotrophic compound that activates the synthesis of endogenous neurotrophins. By promoting the production of neurotrophins such as NGF and BDNF, Paliroden supports neuronal survival, growth, and differentiation. The compound's neurotrophic effects have been characterized in cell-based assays measuring neuronal survival and neurite outgrowth. Paliroden has been shown to be effective in preclinical models of neurodegenerative diseases, including Alzheimer's disease and Parkinson's disease. The compound's ability to cross the blood-brain barrier and its oral bioavailability make it suitable for in vivo studies. Paliroden has been investigated in clinical trials for Alzheimer's disease and Parkinson's disease.
|
| ln Vivo |
Paliroden has been evaluated in vivo in animal models of neurodegenerative diseases and in clinical trials. The compound is an orally active neurotrophic, non-peptidic compound that activates the synthesis of endogenous neurotrophins. In animal models, Paliroden has been shown to promote neuronal survival and function, reducing neurodegeneration and improving cognitive and motor function. The compound has been investigated in clinical trials for Alzheimer's disease and Parkinson's disease. In these trials, Paliroden's safety, tolerability, pharmacokinetics, and efficacy have been assessed. Detailed clinical trial data are available from published studies. Paliroden is for research use only and is not for human therapeutic use.
|
| Enzyme Assay |
Neurotrophin synthesis assays are performed using neuronal cell lines or primary neuronal cultures. Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with Paliroden at various concentrations for 24-72 hours. Neurotrophin levels (e.g., NGF, BDNF) in cell lysates or culture supernatants are measured by ELISA or Western blotting. Neuronal survival is assessed by counting viable neurons or by measuring neurite outgrowth. Gene expression of neurotrophins and their receptors is assessed by qRT-PCR. Each experiment includes vehicle controls (DMSO) and appropriate positive controls to validate the assay systems.
|
| Cell Assay |
Cellular activity of Paliroden is evaluated in neuronal cell lines (e.g., SH-SY5Y, PC12) or primary neuronal cultures. Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with Paliroden at concentrations ranging from 0.1 to 10 μM for 24-72 hours. Cell viability is assessed using MTT or LDH assays. Neurite outgrowth is assessed by microscopy. Neurotrophin levels are measured by ELISA. Neurotrophin receptor signaling is assessed by Western blotting for phosphorylated Trk receptors and downstream signaling components (e.g., ERK, AKT). Each experiment includes vehicle controls (DMSO) and appropriate positive controls (e.g., recombinant NGF or BDNF).
|
| Animal Protocol |
In vivo efficacy of Paliroden is evaluated in animal models of neurodegenerative diseases, including Alzheimer's disease and Parkinson's disease. The compound is administered orally at doses determined by preclinical studies. In Alzheimer's disease models, cognitive function is assessed using behavioral tests (Morris water maze, novel object recognition). Amyloid plaque burden and tau pathology are assessed by immunohistochemistry. In Parkinson's disease models, motor function is assessed using the rotarod test, open field test, and other behavioral tests. Dopaminergic neuron survival is assessed by tyrosine hydroxylase immunohistochemistry. Neurotrophin levels in the brain are measured by ELISA. Sample sizes typically range from 8-12 animals per group.
|
| ADME/Pharmacokinetics |
Molecular Weight: 407.47. Formula: C26H24F3N. CAS No.: 188396-77-2. IUPAC Name: 1-(2-(Biphenyl-4-yl)ethyl)-4-(3-(trifluoromethyl)phenyl)-1,2,3,6-tetrahydropyridine. Synonyms: Paliroden; SR57667B; SR5-7667B. Appearance: Solid. Purity: Typically ≥98%. Solubility: Soluble in DMSO. Storage: Typically at -20°C. Paliroden is an orally active neurotrophic, non-peptidic compound that activates synthesis of endogenous neurotrophins and is indicated for Alzheimer's disease and Parkinson's disease research.
|
| Toxicity/Toxicokinetics |
Paliroden has been evaluated in clinical trials for safety and efficacy. The compound is generally well-tolerated at therapeutic doses. Common adverse effects may include gastrointestinal disturbances, headache, and dizziness. As a neurotrophic compound, potential toxicities may include effects on cell growth and differentiation. Standard toxicology studies have been conducted as part of the clinical development program. The compound has been investigated in Phase II clinical trials for Alzheimer's disease and Parkinson's disease. Regulatory approvals have not been reported.
|
| References | |
| Additional Infomation |
Paliroden is an orally effective non-peptide neurotrophic compound that activates the synthesis of endogenous neurotrophic factors. Studies have shown that Paliroden increases the rate of neural progenitor cell and mature neuron generation. It is indicated for the treatment of Alzheimer's disease and Parkinson's disease.
Drug Indications Studied for the treatment of Alzheimer's disease and Parkinson's disease. Mechanism of Action SR 57667 may be an irreversible MAOB inhibitor. Pharmacodynamics SR 57667 is an orally effective non-peptide neurotrophic compound that activates the synthesis of endogenous neurotrophic factors. Studies have shown that SR 57667 increases the rate of neural progenitor cell and mature neuron generation. Paliroden is also known as SR57667B and SR5-7667B. Its IUPAC name is 1-(2-(Biphenyl-4-yl)ethyl)-4-(3-(trifluoromethyl)phenyl)-1,2,3,6-tetrahydropyridine. Paliroden is an orally active neurotrophic, non-peptidic compound that activates synthesis of endogenous neurotrophins. It is indicated for use in Alzheimer's disease and Parkinson's disease research. Paliroden has been investigated in Phase II clinical trials for these indications. No regulatory approvals have been reported. Paliroden is for research use only. |
| Molecular Formula |
C26H24F3N
|
|---|---|
| Molecular Weight |
407.48
|
| Exact Mass |
407.186
|
| CAS # |
188396-77-2
|
| PubChem CID |
11567682
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
6.642
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
30
|
| Complexity |
555
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC(C1=C([H])C([H])=C([H])C(=C1[H])C1=C([H])C([H])([H])N(C([H])([H])C([H])([H])C2C([H])=C([H])C(C3C([H])=C([H])C([H])=C([H])C=3[H])=C([H])C=2[H])C([H])([H])C1([H])[H])(F)F
|
| InChi Key |
CNEWKIDCGDXBDE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H24F3N/c27-26(28,29)25-8-4-7-24(19-25)23-14-17-30(18-15-23)16-13-20-9-11-22(12-10-20)21-5-2-1-3-6-21/h1-12,14,19H,13,15-18H2
|
| Chemical Name |
1-[2-(4-phenylphenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-pyridine
|
| Synonyms |
SR 57667; SR57667; SR-57667
|
| 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 | 2.4541 mL | 12.2705 mL | 24.5411 mL | |
| 5 mM | 0.4908 mL | 2.4541 mL | 4.9082 mL | |
| 10 mM | 0.2454 mL | 1.2271 mL | 2.4541 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
