WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H329444
CAS#: 134234-12-1 (free base)
Description: Traxoprodil, also known as CP-101606 and CP 98113, is a NR2B N-Methyl-D-Aspartate (NMDA) antagonist potentially for the treatment of major depressive. Traxoprodil potentiates the antidepressant-like effects of certain antidepressant drugs in the forced swim test in mice. Traxoprodil decreases pentylenetetrazol-induced seizures.
Hodoodo Cat#: H329444
Name: Traxoprodil
CAS#: 134234-12-1 (free base)
Chemical Formula: C20H25NO3
Exact Mass: 327.18
Molecular Weight: 327.424
Elemental Analysis: C, 73.37; H, 7.70; N, 4.28; O, 14.66
Related CAS #: 134234-12-1 (free base) 188591-67-5 (mesylate)
Synonym: Traxoprodil; CP-101606; CP101606; CP 101606; CP 98113.
IUPAC/Chemical Name: 1-((1S,2S)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol
InChi Key: QEMSVZNTSXPFJA-HNAYVOBHSA-N
InChi Code: InChI=1S/C20H25NO3/c1-15(19(23)16-7-9-18(22)10-8-16)21-13-11-20(24,12-14-21)17-5-3-2-4-6-17/h2-10,15,19,22-24H,11-14H2,1H3/t15-,19+/m0/s1
SMILES Code: O[C@@H](C1=CC=C(O)C=C1)[C@H](C)N2CCC(C3=CC=CC=C3)(O)CC2
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Related CAS# 134234-12-1 (Traxoprodil free base) 189894-57-3 (Traxoprodil mesylate hydrate)
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 327.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Stasiuk W, Serefko A, Szopa A, Wyska E, Świąder K, Wlaź P, Poleszak E. Traxoprodil augments the antidepressant-like activity of agomelatine but not of mianserin or tianeptine in the forced swim test in mice. Pharmacol Rep. 2016 Oct;68(5):960-3. doi: 10.1016/j.pharep.2016.04.013. PubMed PMID: 27371898.
2: Poleszak E, Stasiuk W, Szopa A, Wyska E, Serefko A, Oniszczuk A, Wośko S, Świąder K, Wlaź P. 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. doi: 10.1007/s11011-016-9810-5. PubMed PMID: 26924124; PubMed Central PMCID: PMC4933725.
3: Naspolini AP, Cocco AR, Villa Martignoni F, Oliveira MS, Furian AF, Rambo LM, Rubin MA, Barron S, Mello CF. Traxoprodil decreases pentylenetetrazol-induced seizures. Epilepsy Res. 2012 Jun;100(1-2):12-9. doi: 10.1016/j.eplepsyres.2012.01.002. PubMed PMID: 22281061.
4: Prakash C, Cui D, Potchoiba MJ, Butler T. Metabolism, distribution and excretion of a selective N-methyl-D-aspartate receptor antagonist, traxoprodil, in rats and dogs. Drug Metab Dispos. 2007 Aug;35(8):1350-64. PubMed PMID: 17496205.
5: Taylor TJ, Diringer K, Russell T, Venkatakrishnan K, Wilner K, Crownover PH, Benincosa LJ, Gibbs MA. Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers. Clin Pharmacokinet. 2006;45(10):989-1001. PubMed PMID: 16984212.
6: Yurkewicz L, Weaver J, Bullock MR, Marshall LF. The effect of the selective NMDA receptor antagonist traxoprodil in the treatment of traumatic brain injury. J Neurotrauma. 2005 Dec;22(12):1428-43. PubMed PMID: 16379581.
7: Johnson K, Shah A, Jaw-Tsai S, Baxter J, Prakash C. Metabolism, pharmacokinetics, and excretion of a highly selective N-methyl-D-aspartate receptor antagonist, traxoprodil, in human cytochrome P450 2D6 extensive and poor metabolizers. Drug Metab Dispos. 2003 Jan;31(1):76-87. PubMed PMID: 12485956.