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Submit ReviewXamoterol hemifumarate
Description: Selective β1 partial agonist
Alternative Names: ICI 118,587
Chemical Name: 1-(4-Hydroxyphenoxy)-3-[2-(4-morpholinocarboxamido)ethylamino]-2-propanol hemifumarate
Purity: ≥97% (HPLC)
Biological Activity for Xamoterol hemifumarate
Xamoterol hemifumarate is a β1-adrenoceptor-selective partial agonist (pA2 values are 7.4 - 7.8 and 5.2 - 6.2 at β1- and β2-adrenoceptors respectively).
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Compound Libraries for Xamoterol hemifumarate
Xamoterol hemifumarate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Xamoterol hemifumarate
| M. Wt | 397.43 |
| Formula | C16H25N3O5.0.5C4H4O4 |
| Storage | Store at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 73210-73-8 |
| PubChem ID | 6440459 |
| InChI Key | QEDVGROSOZBGOZ-WXXKFALUSA-N |
| Smiles | [H]OC(=O)\C=C\C(=O)O[H].OC(CNCCNC(=O)N1CCOCC1)COC1=CC=C(O)C=C1.OC(CNCCNC(=O)N1CCOCC1)COC1=CC=C(O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Xamoterol hemifumarate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 50 | ||
| DMSO | 39.74 | 100 |
Preparing Stock Solutions for Xamoterol hemifumarate
The following data is based on the product molecular weight 397.43. 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 | 2.52 mL | 12.58 mL | 25.16 mL |
| 5 mM | 0.5 mL | 2.52 mL | 5.03 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.52 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets for Xamoterol hemifumarate
References for Xamoterol hemifumarate
References are publications that support the biological activity of the product.
Barlow et al (1981) β-Adrenoceptor stimulant properties of aminoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols. J.Med.Chem. 24 315 PMID: 6115058
Malta et al (1985) The in vitro pharmacology of xamoterol (ICI 118,587). Br.J.Pharmacol. 85 179 PMID: 2862938
Nuttall and Snow (1982) The cardiovascular effects of ICI 118,587: a β1-adrenoceptor partial agonist. Br.J.Pharmacol. 77 381 PMID: 6128041
If you know of a relevant reference for Xamoterol hemifumarate, please let us know.
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10 Citations for Xamoterol hemifumarate
Citations are publications that use Tocris products. Selected citations for Xamoterol hemifumarate include:
Copik et al (2015) Isoproterenol acts as a biased agonist of the α-1A-adrenoceptor that selectively activates the MAPK/ERK pathway. J Pharmacol Exp Ther 10 e0115701 PMID: 25606852
Zhi et al (2019) Adrenergic modulation of AMPK-dependent autophagy by chronic stress enhances cell proliferation and survival in gastric cancer. Int J Oncol 54 1625 PMID: 30896863
Creed et al (2015) β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion. Breast Cancer Res 17 145 PMID: 26607426
Baker et al (2011) Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses. FASEB J 25 4486 PMID: 21865315
Rankovic et al (2011) Modulation of calcium-dependent inactivation of L-type Ca2+ channels via β-adrenergic signaling in thalamocortical relay neurons. PLoS One 6 e27474 PMID: 22164209
Picard et al (2018) Bioluminescence resonance energy transfer-based biosensors allow monitoring of ligand- and transducer-mediated GPCR conformational changes. Commun Biol 1 106 PMID: 30271986
Lavine et al (2013) Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism. JAMA Ophthalmol 131 376 PMID: 23303344
Skeberdis et al (1997) Pharmacological characterization of the receptors involved in the beta-adrenoceptor-mediated stimulation of the L-type Ca2+ current in frog ventricular myocytes. Br J Pharmacol 121 1277 PMID: 9257904
Steinle et al (2003) β 3-adrenergic receptors regulate retinal endothelial cell migration and proliferation. PLoS One 278 20681 PMID: 12670949
Lavine (2017) β2-Adrenergic Receptor Antagonism Attenuates CNV Through Inhibition of VEGF and IL-6 Expression. Invest Ophthalmol Vis Sci 58 299 PMID: 28114591
Do you know of a great paper that uses Xamoterol hemifumarate from Tocris? Please let us know.
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.