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Traxoprodil (Synonyms: CP 98,113)

رقم الكتالوجGC30839

Traxoprodil (CP101،606) هو مضاد فعال وانتقائي لـ NMDA ويحمي الخلايا العصبية في قرن آمون مع IC50 من 10 نانومتر

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Traxoprodil التركيب الكيميائي

Cas No.: 134234-12-1

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
74٫00
متوفر
1mg
27٫00
متوفر
5mg
68٫00
متوفر
10mg
99٫00
متوفر
25mg
216٫00
متوفر
50mg
351٫00
متوفر
100mg
515٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of Traxoprodil

Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.

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].

[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.

Protocol of Traxoprodil

Animal experiment:

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.

Chemical Properties of Traxoprodil

Cas No. 134234-12-1 SDF
المرادفات CP 98,113
Canonical SMILES OC1(C2=CC=CC=C2)CCN([C@@H](C)[C@@H](O)C3=CC=C(O)C=C3)CC1
Formula C20H25NO3 M.Wt 327.42
الذوبان DMSO : ≥ 150 mg/mL (458.13 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Traxoprodil

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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