| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Phenserine (1-25 μM; 48 hours; CHO APP751SW cells): APP levels were reduced by 51.4% in APP-treated CHO APP751SW cells, compared to an 18.6% reduction in cells when treated with 10 μM Phenserine [2]. 2]
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|---|---|
| ln Vivo |
When cholinergic function is compromised, phenesine (1-4 mg/kg; intraperitoneal injection; 4 days duration; Fischer-344-loaded construct) therapy enhances learning in spatial memory tests [3].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: CHO APP751SW Cell Tested Concentrations: 1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM Incubation Duration: 48 hrs (hours) Experimental Results: Cells treated with 10 μM diminished APP levels by 8.6%, while 25 μM concentration diminished APP levels 51.4%%. |
| Animal Protocol |
Animal/Disease Models: 344 male Fischer-scopolamine-induced rats (5 months old) [3]
Doses: 1 mg/kg, 2 mg/kg, 4 mg/kg Route of Administration: intraperitoneal (ip) injection; 4 days Experimental Results: Scopolamine treatment Morris water maze performance improved in rats. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed and cleared from the body. Biological Half-Life 8 to 10 hours |
| References | |
| Additional Infomation |
Phenserine is under development by Axonyx, a US biopharmaceutical company that focuses on treatments for dementia. Phenserine is a next generation acetylcholinesterase (AChE) inhibitor indicated for the treatment of AD. Unlike currently marketed AChE inhibitors, it has a dual mechanism of action that also includes anti-amyloid activity, which may confer disease-modifying effects in patients with AD. If this is substantiated in an ongoing clinical trial then phenserine may open the door to an entirely new type of treatment for AD. Axonyx announced on 20 September 2005 that phenserine was ineffective in two curtailed phase 3 trials.
Drug Indication For the treatment of Alzheimer's disease (AD). Mechanism of Action Phenserine is a highly selective, reversible acetylcholinesterase inhibitor, a mechanism of action known to improve memory and cognition in Alzheimer’s subjects. Phenserine may prove to concentrate in the brain rapidly which would reduce the incidence of drug toxicity and side effects. Pharmacodynamics Phenserine, a phenylcarbamate of physostigmine, is a reversible acetyl-selective cholinesterase inhibitor. In studies of rats with lesions of the forebrain cholinergic system, injections of phenserine was found to significantly decrease the levels of secreted beta-APP in the CSF of the rats. A study on cultured human brain cells found that phenserine reduces Abeta levels by regulating beta-APP translation. |
| Molecular Formula |
C20H23N3O2
|
|---|---|
| Molecular Weight |
337.41552
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| Exact Mass |
337.179
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| CAS # |
101246-66-6
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| Related CAS # |
Buntanetap;116839-68-0
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| PubChem CID |
192706
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.228g/cm3
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| Boiling Point |
468.7ºC at 760mmHg
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| Flash Point |
237.3ºC
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| Vapour Pressure |
5.85E-09mmHg at 25°C
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| Index of Refraction |
1.633
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| LogP |
3.742
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
507
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@]12CCN([C@@H]1N(C3=C2C=C(C=C3)OC(=O)NC4=CC=CC=C4)C)C
|
| InChi Key |
PBHFNBQPZCRWQP-QUCCMNQESA-N
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| InChi Code |
InChI=1S/C20H23N3O2/c1-20-11-12-22(2)18(20)23(3)17-10-9-15(13-16(17)20)25-19(24)21-14-7-5-4-6-8-14/h4-10,13,18H,11-12H2,1-3H3,(H,21,24)/t18-,20+/m1/s1
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| Chemical Name |
[(3aR,8bS)-3,4,8b-trimethyl-2,3a-dihydro-1H-pyrrolo[2,3-b]indol-7-yl] N-phenylcarbamate
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~592.73 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (14.82 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 50.0 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: ≥ 5 mg/mL (14.82 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 50.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
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