Xamoterol hemifumarate
| Code | Size | Price |
|---|
| AG-CR1-3536-M001 | 1 mg | £35.00 |
Quantity:
| AG-CR1-3536-M005 | 5 mg | £85.00 |
Quantity:
| AG-CR1-3536-M025 | 25 mg | £300.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
AMBIENT
Storage:
Short Term: +4°C, Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
ICI 118587
Appearance:
White to off-white powder.
CAS:
73210-73-8
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS08
Handling Advice:
Keep cool and dry.
Hazards:
H361
InChi:
InChI=1S/C16H25N3O5.C4H4O4/c20-13-1-3-15(4-2-13)24-12-14(21)11-17-5-6-18-16(22)19-7-9-23-10-8-19;5-3(6)1-2-4(7)8/h1-4,14,17,20-21H,5-12H2,(H,18,22);1-2H,(H,5,6)(H,7,8)/b;2-1+
InChiKey:
LVVMVDRJXOBQNA-WLHGVMLRSA-N
Long Description:
Chemical. CAS: 73210-73-8. Formula: C16H25N3O5 • 1/2C4H4O4. MW: 339.4 . 58.0. Soluble in water (20mg/ml) or DMSO (40mg/ml). A phenoxypropanolamine derivative that is a selective partial agonist of beta1-adrenergic receptors (beta1-ARs) (pA2 values are 7.4 - 7.8 and 5.2 - 6.2 at beta1- and beta2-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 beta2-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 beta1-AR antagonist betaxolol but not the selective beta2-AR antagonist ICI 118551.
MDL:
MFCD00661104
Molecular Formula:
C16H25N3O5 • 1/2C4H4O4
Molecular Weight:
339.4 . 58.0
Package Type:
Vial
Precautions:
P280, P308+313
Product Description:
A phenoxypropanolamine derivative that is a selective partial agonist of beta1-adrenergic receptors (beta1-ARs) (pA2 values are 7.4 - 7.8 and 5.2 - 6.2 at beta1- and beta2-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 beta2-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 beta1-AR antagonist betaxolol but not the selective beta2-AR antagonist ICI 118551.
Purity:
>98% (NMR)
Signal word:
Warning
SMILES:
O=C(NCC[NH2+]CC(O)COC1=CC=C(O)C=C1)N2CCOCC2.[O-]C(/C=C/C(O)=O)=O
Solubility Chemicals:
Soluble in water (20mg/ml) or DMSO (40mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
beta-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 beta1-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 beta-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)