[CAS NO. 101246-66-6] Phenserine
PRODUCTS SPECIFICATIONS [101246-66-6]
DESCRIPTION [101246-66-6]
Overview
| MDL | MFCD00672748 |
|---|---|
| Molecular Weight | 337.42 |
| Molecular Formula | C20H23N3O2 |
| SMILES | CN1[C@](N(C)CC2)([H])[C@]2(C)C3=C1C=CC(OC(NC4=CC=CC=C4)=O)=C3 |
Summary
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease [1] [2] [3] .
IC50 & Target
AChE; β-amyloid precursor protein; β-amyloid peptide [1]
In Vitro
Phenserine (1-25 μM; 48 hours; CHO APP 751SW cells) treatment CHO APP 751SW cell shows 18.6% reduction in cells treated with 10 μM of Phenserine, while 25 μM concentration of Phenserine reduces APP level by 51.4% [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [2]
| Cell Line: | CHO APP 751SW cells |
| Concentration: | 1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM |
| Incubation Time: | 48 hours |
| Result: | 8.6% reduction in cells treated with 10 μM, while 25 μM concentration reduces APP level by 51.4%. |
In Vivo
Phenserine (1-4 mg/kg; intraperitoneal injection; for 4 days; male Fischer-344 rats) treatment improves learning when cholinergic function has been impaired in a spatial memory task [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Fischer-344 rats (5 months old) induced by scopolamine [3] |
| Dosage: | 1 mg/kg, 2 mg/kg, 4 mg/kg |
| Administration: | Intraperitoneal injection; for 4 days |
| Result: | Improved morris water maze performance of scopolamine-treated rats.. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 200 mg/mL ( 592.73 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9637 mL | 14.8183 mL | 29.6367 mL |
| 5 mM | 0.5927 mL | 2.9637 mL | 5.9273 mL |
| 10 mM | 0.2964 mL | 1.4818 mL | 2.9637 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (14.82 mM); Clear solution
References
- [1] Klein J. Phenserine. Expert Opin Investig Drugs. 2007 Jul;16(7):1087-97.
- [2] Asuni AA, et al. Modulation of amyloid precursor protein expression reduces β-amyloid deposition in a mouse model. Ann Neurol. 2014 May;75(5):684-99.
- [3] Janas AM, et al. The cholinesterase inhibitor, phenserine, improves Morris water maze performance of scopolamine-treated rats. Life Sci. 2005 Jan 21;76(10):1073-81.
Synonyms
