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[CAS NO. 134234-12-1] Traxoprodil
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-W018061 |
| Brand: | MCE |
| CAS: | 134234-12-1 |
Overview
| MDL | MFCD00926469 |
|---|---|
| Molecular Weight | 327.42 |
| Molecular Formula | C20H25NO3 |
| SMILES | OC1(C2=CC=CC=C2)CCN([C@@H](C)[C@@H](O)C3=CC=C(O)C=C3)CC1 |
1 Publications Citing Use of MCE
Summary
Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC 50 of 10 nM.
IC50 & Target
IC50: 10 nM (Neuroprotection) [1]
In Vivo
Traxoprodil is potent at blocking haloperidol-induced catalepsy and with an ED 50 less than 1 mg/kg. Traxoprodil is effective at 1 mg/kg to block NMDA (ip) stimulated cfos induction in mice [1] . Traxoprodil at a dose of 20 and 40 mg/kg exhibits antidepressant activity in the Forced swim test and it is not related to changes in animals’ locomotor activity [2] . Traxoprodil (20 nM i.c.v.) increases the latency to generalized tonic-clonic seizures induced by PTZ (70 mg/kg; i.p.). Traxoprodil (60 mg/kg, p.o.) increases the latency to clonic and generalized seizures, and decreases the total time spent in seizures [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00163085 | Pfizer |
Parkinson´s Disease
|
May 2005 | Phase 2 |
| NCT00163059 | Pfizer |
Depressive Disorder, Major
|
May 2004 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 62.5 mg/mL ( 190.89 mM ; Need ultrasonic)
H 2 O : 0.1 mg/mL ( 0.31 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.0542 mL | 15.2709 mL | 30.5418 mL |
| 5 mM | 0.6108 mL | 3.0542 mL | 6.1084 mL |
| 10 mM | 0.3054 mL | 1.5271 mL | 3.0542 mL |
References
- [1] Chenard BL, et al. (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses. J Med Chem. 1995 Aug 4;38(16):3138-45.
- [2] Poleszak E, et al. Traxoprodil, a selective antagonist of the NR2B subunit of the NMDA receptor, potentiates the antidepressant-like effects of certain antidepressant drugs in the forced swim test in mice. Metab Brain Dis. 2016 Aug;31(4):803-14.
- [3] Naspolini AP, et al. Traxoprodil decreases pentylenetetrazol-induced seizures. Epilepsy Res. 2012 Jun;100(1-2):12-9.
Synonyms
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