WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319871
CAS#: 98819-76-2
Description: Esreboxetine, also known as PNU-165442 and (S,S)-Reboxetine, is a selective norepinephrine reuptake inhibitor which was under development by Pfizer for the treatment of neuropathic pain and fibromyalgia but failed to show significant benefit over currently available medications and was discontinued. It is the (+)-(S,S)-enantiomer of reboxetine and is even more selective in comparison. However, recently it has been shown that esreboxetine could be effective in fibromyalgia patients.
Hodoodo Cat#: H319871
Name: Esreboxetine
CAS#: 98819-76-2
Chemical Formula: C19H23NO3
Exact Mass: 313.17
Molecular Weight: 313.397
Elemental Analysis: C, 72.82; H, 7.40; N, 4.47; O, 15.32
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Synonym: PNU-165442; PNU 165442; PNU165442; (S,S)-Reboxetine; Esreboxetine
IUPAC/Chemical Name: (S)-2-((S)-(2-ethoxyphenoxy)(phenyl)methyl)morpholine
InChi Key: CBQGYUDMJHNJBX-OALUTQOASA-N
InChi Code: InChI=1S/C19H23NO3/c1-2-21-16-10-6-7-11-17(16)23-19(15-8-4-3-5-9-15)18-14-20-12-13-22-18/h3-11,18-20H,2,12-14H2,1H3/t18-,19-/m0/s1
SMILES Code: CCOC1=CC=CC=C1O[C@H]([C@@H]2CNCCO2)C3=CC=CC=C3
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, not in water
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 313.40 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: Fujimori I, Yukawa T, Kamei T, Nakada Y, Sakauchi N, Yamada M, Ohba Y,
Takiguchi M, Kuno M, Kamo I, Nakagawa H, Hamada T, Igari T, Okuda T, Yamamoto S,
Tsukamoto T, Ishichi Y, Ueno H. Design, synthesis and biological evaluation of a
novel series of peripheral-selective noradrenaline reuptake inhibitor. Bioorg Med
Chem. 2015 Aug 1;23(15):5000-14. doi: 10.1016/j.bmc.2015.05.017. Epub 2015 May
15. PubMed PMID: 26051602.
2: Shen F, Tsuruda PR, Smith JA, Obedencio GP, Martin WJ. Relative contributions
of norepinephrine and serotonin transporters to antinociceptive synergy between
monoamine reuptake inhibitors and morphine in the rat formalin model. PLoS One.
2013 Sep 30;8(9):e74891. doi: 10.1371/journal.pone.0074891. eCollection 2013.
PubMed PMID: 24098676; PubMed Central PMCID: PMC3787017.
3: Arnold LM, Hirsch I, Sanders P, Ellis A, Hughes B. Safety and efficacy of
esreboxetine in patients with fibromyalgia: a fourteen-week, randomized,
double-blind, placebo-controlled, multicenter clinical trial. Arthritis Rheum.
2012 Jul;64(7):2387-97. doi: 10.1002/art.34390. PubMed PMID: 22275142.
4: Arnold LM, Chatamra K, Hirsch I, Stoker M. Safety and efficacy of esreboxetine
in patients with fibromyalgia: An 8-week, multicenter, randomized, double-blind,
placebo-controlled study. Clin Ther. 2010 Aug;32(9):1618-32. doi:
10.1016/j.clinthera.2010.08.003. PubMed PMID: 20974319.
5: Klarskov N, Scholfield D, Soma K, Darekar A, Mills I, Lose G. Measurement of
urethral closure function in women with stress urinary incontinence. J Urol. 2009
Jun;181(6):2628-33; discussion 2633. doi: 10.1016/j.juro.2009.01.114. Epub 2009
Apr 16. PubMed PMID: 19375093.