[CAS NO. 519187-97-4] Edonerpicmaleate
PRODUCTS SPECIFICATIONS [519187-97-4]
DESCRIPTION [519187-97-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 407.48 |
| Molecular Formula | C20H25NO6S |
| SMILES | OC1CN(CCCOCCC2=CC=C3C(C=CS3)=C2)C1.O=C(O)/C=C\C(O)=O |
Summary
Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides ( Aβ ).
IC50 & Target
amyloid-β peptides [1]
In Vitro
Edonerpic maleate (T-817MA) treatment preserves the cortical neurons in the presence of Aβ(1-42). Twenty-four hours of pretreatment, followed by the continuous presence of Edonerpic maleate, prevents oxidative stress-induced neuronal death at 0.1 and 1 μM. Edonerpic maleate almost completely prevents GSH reduction at 0.1 and 1 μM. Hippocampal slices with 1 μM Edonerpic maleate treatment generate more and much longer neurites than control slices. Edonerpic maleate significantly increases the neurite length at 0.1 and 1 μM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The post hoc test indicates that the mean density of PSA-positive cells is significantly larger in the vehicle and Aβ infusion+high-dose Edonerpic maleate (T-817MA) groups than that in the Aβ infusion control group (P<0.01). The results indicate that the vehicle and Aβ infusion+high-dose Edonerpic maleate groups display efficient learning in the place learning task (PLT), while these two groups also display vigorous neurogenesis. Treatment with Edonerpic maleate and donepezil does not increase the mean density of normal granule cells; there are no significant differences in the mean granule cell density among the Aβ infusion control, Aβ infusion+high-dose Edonerpic maleate, Aβ infusion+low-dose Edonerpic maleate and Aβ infusion+donepezil groups [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00663936 | FUJIFILM Toyama Chemical Co., Ltd. |
Alzheimer´s Disease
|
April 2008 | Phase 2 |
| NCT04191486 | FUJIFILM Toyama Chemical Co., Ltd. |
Mild Cognitive Impairment
|
December 24, 2019 | Phase 2 |
| NCT02693197 | FUJIFILM Toyama Chemical Co., Ltd.|Celerion |
Healthy|Hepatic Impairment
|
February 2016 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 245.41 mM ; Need ultrasonic)
H 2 O : 100 mg/mL ( 245.41 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: PBS
Solubility: 140 mg/mL (343.58 mM); Clear solution; Need ultrasonic
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution
-
3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution
References
- [1] Hirata K, et al. A novel neurotrophic agent, T-817MA [1-{3-[2-(1-benzothiophen-5-yl) ethoxy] propyl}-3-azetidinol maleate], attenuates amyloid-beta-induced neurotoxicity and promotes neurite outgrowth in rat cultured central nervous system neurons. J Phar
- [2] Kimura T, et al. T-817MA, a neurotrophic agent, ameliorates the deficits in adult neurogenesis and spatial memory in rats infused i.c.v. with amyloid-beta peptide. Br J Pharmacol. 2009 Jun;157(3):451-63.