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Traxoprodil

  Cat. No.:  DC8824   Featured
Chemical Structure
134234-12-1
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Field of application
Traxoprodil is an NMDA ε 2 (NR2B) antagonist that has been studied as an alternative to serotonin selective reuptake inhibitors.
Cas No.: 134234-12-1
Chemical Name: 1-((1S,2S)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol
Synonyms: CP-101,606,CP 101606,CP101606
SMILES: C[C@@H]([C@H](C1=CC=C(C=C1)O)O)N2CCC(CC2)(C3=CC=CC=C3)O
Formula: C20H25NO3
M.Wt: 327.42
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
Target: IC50: 10 nM (Neuroprotection)[1]
In Vivo: Traxoprodil is potent at blocking haloperidol-induced catalepsy and with an ED50 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].
Animal Administration: Rats[3] The effect of traxoprodil and SPD on PTZ-induced seizures is investigated by injecting the Adult (90-100 days-old) male Wistar rats (250-300 g) with traxoprodil (0.2, 2 or 20 nM/site), SPD (0.02, 0.2 or 2 nM/site), or with vehicle (0.9% NaCl, 1 μL) 15 min before the administration of PTZ (35 or 70 mg/kg, i.p.)[3]. Mice[2] The Forced swim test is done on male Albino Swiss mice (25-30 g). Traxoprodil (5, 10, 20, 40 mg/kg), imipramine and saline are administered i.p. 60 min before the test. The antidepressant activity is measured[2].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC8824 Traxoprodil Traxoprodil is an NMDA ε 2 (NR2B) antagonist that has been studied as an alternative to serotonin selective reuptake inhibitors.
DC8175 Rapastinel(GLYX-13) Rapastinel(GLYX-13) is a NMDA receptor partial agonist that acts at the glycine site.
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