| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
DJ-1 protein. By binding to DJ-1, it protects the protein from oxidative damage, thereby preserving its neuroprotective function.
|
|---|---|
| ln Vitro |
In vitro, Protein deglycase DJ-1 against-1 is a DJ-1 binding compound that selectively targets DJ1. It prevents DJ-1 over-oxidation, which would otherwise impair its protective function. This activity can be assessed in cell-based models of oxidative stress to measure its neuroprotective efficacy.
|
| ln Vivo |
The MPTP-induced locomotion, dopaminergic neuron cell death, and dopamine content were dramatically recovered by protein deglycase DJ-1 against-1 (Compound 23; 1 mg/kg; i.p.; one hour pretreatment; daily; for 4 days), but not in DJ-1(-/-) mice[1].
In MPTP-induced Parkinson's disease mouse models, intraperitoneal injection of compound 23 at 1 mg/kg for 4 consecutive days improves motor deficits, protects dopaminergic neurons, and restores dopamine levels. These effects are dependent on the presence of the DJ-1 protein, as they were not observed in DJ-1-deficient mice. |
| Enzyme Assay |
The binding of Protein deglycase DJ-1 against-1 to DJ-1 protein can be assessed using techniques like Surface Plasmon Resonance (SPR) or Isothermal Titration Calorimetry (ITC) to determine the binding affinity and kinetics. The specificity of binding can be confirmed using competition assays with other proteins.
|
| Cell Assay |
To evaluate its neuroprotective effects, neuronal cell lines (e.g., SH-SY5Y) are treated with the compound and then exposed to an oxidative stressor like H2O2 or MPTP. Cell viability is measured using assays like MTT. Markers of oxidative stress and DJ-1 oxidation status are analyzed via Western blot to confirm the compound's mechanism of action.
|
| Animal Protocol |
Animal/Disease Models: Wild-type male C57BL/6 mice at 8, 11-12 and 9-12 weeks; DJ-1-knockout male mice at 11-13 weeks[1]
Doses: 1 mg/kg Route of Administration: IP; pretreatment one hour; daily; for 4 days Experimental Results: Dramatically restored MPTP (30 mg/kg; IP; One hour after injection) induced locomotion, dopaminergic neuronal cell death and dopamine content in DJ-1(+/+) mice but not in DJ- 1(-/-) mice. The in vivo efficacy of Protein deglycase DJ-1 against-1 is evaluated in the MPTP-induced mouse model of Parkinson's disease. MPTP is administered to mice to induce dopaminergic neuron loss and motor deficits. The compound is then administered intraperitoneally at 1 mg/kg for 4 consecutive days. Motor function is assessed using behavioral tests (e.g., rotarod, open field), and dopaminergic neuron survival is quantified by immunohistochemistry for tyrosine hydroxylase (TH). |
| ADME/Pharmacokinetics |
Pharmacokinetic data for this compound are limited. It is known to penetrate the blood-brain barrier (BBB), which is a critical property for a central nervous system (CNS) drug candidate. It is soluble in DMSO (16 mg/mL) and is typically formulated for in vivo studies using a mixture of DMSO, PEG300, Tween 80, and saline.
|
| Toxicity/Toxicokinetics |
Specific toxicity data are not widely available. However, as a neuroprotective agent targeting DJ-1, it is expected to have a favorable safety profile. Standard safety pharmacology and toxicology studies would be required for clinical development. In vitro assays may show low cytotoxicity.
|
| References | |
| Additional Infomation |
Protein deglycase DJ-1 against-1 is a research compound being investigated for its potential in treating Parkinson's disease. Its ability to penetrate the BBB and protect DJ-1 from oxidative stress positions it as a promising neuroprotective strategy. It is not currently approved for clinical use and is primarily used in preclinical research.
|
| Molecular Formula |
C24H23N3O4
|
|---|---|
| Molecular Weight |
417.4571
|
| Exact Mass |
417.168
|
| CAS # |
724737-74-0
|
| PubChem CID |
983464
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.5
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
31
|
| Complexity |
583
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=CC=CN2C1=NC(=C2)C3=CC=C(C=C3)NC(=O)C4=CC(=C(C(=C4)OC)OC)OC
|
| InChi Key |
DRVIKYTZILDXIS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H23N3O4/c1-15-6-5-11-27-14-19(26-23(15)27)16-7-9-18(10-8-16)25-24(28)17-12-20(29-2)22(31-4)21(13-17)30-3/h5-14H,1-4H3,(H,25,28)
|
| Chemical Name |
3,4,5-trimethoxy-N-[4-(8-methylimidazo[1,2-a]pyridin-2-yl)phenyl]benzamide
|
| 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: 25 mg/mL (59.89 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3954 mL | 11.9772 mL | 23.9544 mL | |
| 5 mM | 0.4791 mL | 2.3954 mL | 4.7909 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3954 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
