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AdipoGen Life Sciences
Xamoterol hemifumarate
30
CHF
CHF 30.00
In stock
AG-CR1-3536-M0011 mgCHF 30.00
AG-CR1-3536-M0055 mgCHF 110.00
AG-CR1-3536-M02525 mgCHF 370.00
| Product Details | |
|---|---|
| Synonyms | ICI 118587 |
| Product Type | Chemical |
| Properties | |
| Formula |
C16H25N3O5 • 1/2C4H4O4 |
| MW | 339.4 . 58.0 |
| CAS | 73210-73-8 |
| Purity Chemicals | ≥98% (NMR) |
| Appearance | White to off-white powder. |
| Solubility | Soluble in water (20mg/ml) or DMSO (40mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | LVVMVDRJXOBQNA-WLHGVMLRSA-N |
| Smiles | O=C(NCC[NH2+]CC(O)COC1=CC=C(O)C=C1)N2CCOCC2.[O-]C(/C=C/C(O)=O)=O |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- A phenoxypropanolamine derivative that is a selective partial agonist of β1-adrenergic receptors (β1-ARs) (pA2 values are 7.4 - 7.8 and 5.2 - 6.2 at β1- and β2-adrenoceptors, respectively), and has shown to improve systolic and diastolic function in studies with heart failure patients. It modulates the sympathetic control of the heart but has no agonist action on β2-adrenoceptors.
- Xamoterol has an EC50 value of 80nM for the generation of cyclic AMP (cAMP) in neonatal rat cardiomyocyte cultures. It increases spontaneous contraction of isolated rat right atria (EC50 = 4.67nM). In vivo, xamoterol increases heart rate, an effect that is reversed by the selective β1-AR antagonist betaxolol but not the selective β2-AR antagonist ICI 118551.
Product References
- β-Adrenoceptor stimulant properties of aminoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols: J.J. Barlow, et al.; J. Med. Chem. 24, 315 (1981)
- The cardiovascular effects of ICI 118,587: A β1-adrenoceptor partial agonist: A. Nuttall & H.M. Snow; Br. J. Pharmacol. 77, 381 (1982)
- The in vitro pharmacology of xamoterol (ICI 118,587): E. Malta, et al.; Br. J. Pharmacol. 85, 179 (1985)
- Comparison of the effects of xamoterol and isoprenaline on rat cardiac β-adrenoceptors. Studies of function and regulation: M.T. Kowalski, et al.; Br. J. Pharmacol. 99, 27 (1990)
- The xamoterol experience in the treatment of heart failure:. J.M. Cruickshank, et al.; Am. J. Cardiol. 71, 61C (1993) (Review)
- In vitro and in vivo characterization of intrinsic sympathomimetic activity in normal and heart failure rats: R.N. Willette, et al.; J. Pharmacol. Exp. Ther. 289, 48 (1999)