| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary targets of DB-959 are PPARδ and PPARγ. It acts as a dual agonist at these nuclear receptors. This dual activation regulates genes involved in glucose and lipid metabolism, as well as inflammation. It overcomes the CNS exposure limitations of conventional PPAR agonists, making it suitable for neurodegenerative disease research.
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|---|---|
| ln Vitro |
DB-959 is a potent dual PPARδ/γ agonist. It improves spatial learning and memory in streptozotocin-induced mouse models of cognitive impairment. The compound is orally active and has potential for Alzheimer's disease research. Detailed EC50 values for PPAR activation are not consistently reported but its efficacy in cognitive models is established.
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| ln Vivo |
The impairment of motor function caused by STZ can be restored in STZ-mediated Long Evans rats by administering PPARδ/γ agonist 1 (1 mg/kg; i.g., daily for 16 days) [1].
In vivo, DB-959 improves spatial learning and memory in streptozotocin-induced mouse models of cognitive impairment. It is orally active and has potential for the treatment of Alzheimer's disease. The compound overcomes the CNS exposure limitations of conventional PPAR agonists. Detailed pharmacokinetic and efficacy data are limited but its cognitive benefits are demonstrated. |
| Enzyme Assay |
For non-cellular binding studies, recombinant PPARδ and PPARγ ligand-binding domains are incubated with DB-959 in the presence of a fluorescent PPAR ligand. Binding is measured by fluorescence polarization. EC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cell experiments employ cells expressing PPARδ/γ. Receptor activation is measured by reporter gene assays. Glucose uptake and lipid metabolism are assessed in adipocytes or hepatocytes. These protocols are for reference use only.
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| Animal Protocol |
Animal/Disease Models: STZ-mediated Long Evans rat [1]
Doses: 1 mg/kg Route of Administration: po (oral gavage); one time/day for 16 days Experimental Results: STZ-mediated performance of rats was improved, and pellet cells and Purkinje cells are neuroprotective. Animal studies employ streptozotocin-induced mouse models of cognitive impairment. DB-959 is administered orally, and spatial learning and memory are assessed using the Morris water maze. These protocols are for reference use only. All products are for research use only. |
| References | |
| Additional Infomation |
LY-2624803 is being studied in the clinical trial NCT01236105 (the effects of activated charcoal and administration time on the pharmacokinetics of LY2624803 in healthy subjects).
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| Molecular Formula |
C25H27NO5
|
|---|---|
| Exact Mass |
379.189
|
| CAS # |
1257641-15-8
|
| PubChem CID |
11567064
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
0.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
28
|
| Complexity |
598
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(O)C[C@@H]1CCC2=C1C=CC(OCCC3=C(CC)OC(C4=CC=C(OC)C=C4)=N3)=C2
|
| InChi Key |
UEFWDVMEDFCHGW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H25N3O3/c1-22(2,21(26)27)15-24-11-13-25(14-12-24)20-16-7-3-5-9-18(16)28-19-10-6-4-8-17(19)23-20/h3-10H,11-15H2,1-2H3,(H,26,27)
|
| Chemical Name |
3-(4-benzo[b][1,4]benzoxazepin-6-ylpiperazin-1-yl)-2,2-dimethylpropanoic acid
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| 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
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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.) |
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
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