| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
IP7e targets Nurr1 (nuclear receptor related 1), a transcription factor involved in the regulation of dopaminergic neuron development and function. It is a potent activator of Nurr1 with an EC50 of 3.9 nM. By activating Nurr1, it may exert neuroprotective and anti-inflammatory effects. Some sources also describe IP7e as a selective inhibitor of casein kinase 1 (CK1).
|
|---|---|
| ln Vitro |
IP7e is a potent Nurr1 activator with an EC50 of 3.9 nM. It suppresses NF-κB signaling. Its activity has been confirmed in various in vitro assays. It is a brain-penetrant compound, indicating it can cross the blood-brain barrier to reach its targets in the central nervous system.
|
| ln Vivo |
Prophylactic treatment with IP7e (isoxazolopyridone 7e; 10 mg/kg; oral gavage; twice daily) lowers the incidence and incidence of experimental autoimmune encephalomyelitis (EAE) in a mouse model of MS. severity. IP7e alleviates inflammation and neurodegeneration in the spinal cord of EAE mice through NF-kB pathway-dependent processes [2].
IP7e delays onset and reduces severity of symptoms in mice with experimental autoimmune encephalomyelitis (EAE). It attenuates inflammation and neurodegeneration in spinal cords of EAE mice by an NF-κB pathway-dependent process. Its ability to activate Nurr1 and suppress NF-κB signaling contributes to its neuroprotective and anti-inflammatory effects. |
| Enzyme Assay |
The primary in vitro assays for IP7e include Nurr1 activation assays, where its ability to activate Nurr1-mediated transcription is measured using reporter gene assays. Its EC50 of 3.9 nM is determined from dose-response curves. NF-κB signaling assays measure its ability to suppress NF-κB activation.
|
| Cell Assay |
Cellular assays for IP7e involve treating cells with the compound and measuring its effects on Nurr1 activation and NF-κB signaling. Its ability to activate Nurr1 target gene expression can be assessed by qPCR. Its effects on NF-κB activity can be measured using reporter gene assays or by assessing the expression of NF-κB target genes.
|
| Animal Protocol |
Animal/Disease Models: Experimental autoimmune encephalomyelitis (EAE) female C57BL/6J mice (6-8 weeks old) [2].
Doses: 10 mg/kg Route of Administration: po (oral gavage); twice (two times) daily; prophylactic (before disease onset) 7 to 23 dpi, therapeutic (after disease onset) 21 to 36 dpi Experimental Results: Prophylactic The drug delayed the onset of EAE, diminished the incidence and severity of EAE, and diminished neuroinflammation and histopathological changes. Spinal cord of treated EAE mice. In contrast, the course of EAE is not affected by treatment administration. In vivo animal experiments for IP7e have been conducted using the experimental autoimmune encephalomyelitis (EAE) mouse model, a model of multiple sclerosis. IP7e was administered to mice, and its effects on disease onset, severity, and neuroinflammation were assessed. The compound delayed onset and reduced symptom severity. |
| ADME/Pharmacokinetics |
IP7e has a molecular weight of 390.43 g/mol and a molecular formula of C23H22N2O4. It is soluble in DMSO (39.04 mg/mL). It is a brain-penetrant and orally active compound. It is a potent Nurr1 activator with an EC50 of 3.9 nM.
|
| Toxicity/Toxicokinetics |
The toxicological profile of IP7e is not extensively detailed in the provided sources. As a research compound, it is not intended for human use. Standard safety precautions should be followed when handling. Its safety would need to be established through preclinical studies if it were to be developed for therapeutic applications.
|
| References |
|
| Additional Infomation |
IP7e is a potent, brain-penetrant, and orally active Nurr1 activator with an EC50 of 3.9 nM. It delays onset and reduces severity of symptoms in mice with experimental autoimmune encephalomyelitis (EAE). IP7e suppresses NF-κB signaling. It is available from various chemical suppliers for research purposes.
|
| Molecular Formula |
C23H22N2O4
|
|---|---|
| Molecular Weight |
390.43
|
| Exact Mass |
390.157
|
| CAS # |
500164-74-9
|
| PubChem CID |
9908426
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
611.8±55.0 °C at 760 mmHg
|
| Flash Point |
323.8±31.5 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.593
|
| LogP |
2.61
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
581
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1C(=CC2=C(C1=O)C(=NO2)C3=CC=CC=C3)C4=CC=C(C=C4)COCCOC
|
| InChi Key |
YCAACZFPADQMAR-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H22N2O4/c1-25-19(17-10-8-16(9-11-17)15-28-13-12-27-2)14-20-21(23(25)26)22(24-29-20)18-6-4-3-5-7-18/h3-11,14H,12-13,15H2,1-2H3
|
| Chemical Name |
6-[4-(2-methoxyethoxymethyl)phenyl]-5-methyl-3-phenyl-[1,2]oxazolo[4,5-c]pyridin-4-one
|
| Synonyms |
IP-7e; IP 7e; IP7e
|
| 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 : ~100 mg/mL (~256.13 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.40 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 25.0 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 | 2.5613 mL | 12.8064 mL | 25.6128 mL | |
| 5 mM | 0.5123 mL | 2.5613 mL | 5.1226 mL | |
| 10 mM | 0.2561 mL | 1.2806 mL | 2.5613 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
