Traxoprodil - iGluR Antagonist - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETraxoprodilCat. No.: HY-W018061CAS No.: 134234-12-1分式: CHNO分量: 327.42作靶點: iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 150 m

2、g/mL (458.13 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.0542 mL 15.2709 mL 30.5418 mL5 mM 0.6108 mL 3.0542 mL 6.1084 mL10 mM 0.3054 mL 1.5271 mL 3.0542 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Traxoprodil (CP101,606)種有效

3、的和選擇性的 NMDA 拮抗劑，保護海馬神經(jīng)元的 IC50 值為10 nM。IC50 & Target IC50: 10 nM (Neuroprotection) 1體內(nèi)研究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 a1/2 Ma

4、ster of Small Molecules 您邊的抑制劑師www.MedChemEdose of 20 and 40 mg/kg exhibits antidepressant activity in the Forced swim test and it is not related tochanges in animals locomotor activity 2. Traxoprodil (20 nM i.c.v.) increases the latency to generalizedtonic-clonic seizures induced by PTZ (70 mg/kg;

5、i.p.). Traxoprodil (60 mg/kg, p.o.) increases the latency toclonic and generalized seizures, and decreases the total time spent in seizures 3.PROTOCOLAnimal Rats 3Administration 23 The effect of traxoprodil and SPD on PTZ-induced seizures is investigated by injecting the Adult (90-100days-old) male

6、Wistar rats (250-300 g) with traxoprodil (0.2, 2 or 20 nM/site), SPD (0.02, 0.2 or 2 nM/site), orwith vehicle (0.9% NaCl, 1 L) 15 min before the administration of PTZ (35 or 70 mg/kg, i.p.) 3.Mice 2The Forced swim test is done on male Albino Swiss mice (25-30 g). Traxoprodil (5, 10, 20, 40 mg/kg),im

7、ipramine and saline are administered i.p. 60 min before the test. The antidepressant activity is measured2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chenard BL, et al. (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-pro

8、panol: a potent new neuroprotectant whichblocks 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-likeeffects 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.McePdfHeightCaution: Product has not been fully validated for medical app