Xamoterol hemifumarate
Based on 1 Customer Validation
Xamoterol (Corwin; ICI 118587) hemifumarate is an orally active and selective β1-adrenoceptor partial agonist. Xamoterol hemifumarate acts as agonist at low sympathetic tone, antagonist at high sympathetic tone, with context-dependent cardiovascular effects including modulated heart rate, blood pressure, and cardiac output. Xamoterol hemifumarate can be used for the research of heart failure, postural hypotension, and ischemic heart disease.
For research use only. We do not sell to patients.
- Purity: 98.18%
- CAS No.: 73210-73-8
- Formula: C20H29N3O9
- Molecular Weight:397.43
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Biological Activity
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β1 adrenoceptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
100 μM
Compound: Xamoterol
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Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
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[PMID: 23614528] |
Xamoterol (0.5 nM-50 μM; 2 min) hemifumarate produces weak β2-adrenoceptor-mediated relaxant effects in progesterone-pretreated rat uterus, and non-specific, non-β-adrenoceptor-mediated inhibitory effects in guinea-pig ileal and tracheal preparations, with no β-adrenoceptor-mediated activity in oestrogen-pretreated uterine or rat vas deferens preparations[2].
Xamoterol (70 min) hemifumarate displays selective affinity for β1-adrenoceptors, with a pKD of 7.25 in guinea-pig left atrial membranes (β1) and a pKD of 5.24 in guinea-pig uterine membranes (β2), representing a 100-fold preference for β1 sites[2].
Xamoterol (0.2 nM-6 μM) hemifumarate acts as a β1-selective partial agonist in isolated male AP rat right atria, producing a maximal rate stimulation response 65-70% that of isoprenaline with an EC50 of 4.67 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Xamoterol (600 μg/kg/h; s.c.; continuous infusion; 6 days) hemifumarate does not induce cardiac β-adrenoceptor down-regulation or alter receptor-adenylate cyclase coupling in normal rats[3].
Xamoterol hemifumarate acts as a β1-adrenoceptor partial agonist in anaesthetised areflexic dogs, demonstrating 43% of isoprenaline's intrinsic sympathomimetic activity at β1-receptors without β2-receptor stimulation[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AS rats (200-300 g)[3]
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Dosage:600 μg/kg/h
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Administration:s.c.; continuous infusion; 6 days
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Result:Did not alter the density of total, β1, or β2 cardiac β-adrenoceptors compared to saline control; total Bmax was 17.2 fmol/mg protein (0% change from control), β1 Bmax was 11.8 fmol/mg protein (0% change), and β2 Bmax was 5.3 fmol/mg protein (+8.0% change, not significant).
Left the equilibrium dissociation constant (Kd) of [125I]-pindolol binding unchanged at 38 pM.
Did not significantly modify the effect of Gpp(NH)p on isoprenaline displacement of [125I]-pindolol binding, indicative of β-adrenoceptor-adenylate cyclase coupling.
Resulted in a plasma xamoterol level of 161 nM at the end of the infusion.
Chemical Information
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CAS No. 73210-73-8
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Appearance Solid
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Molecular Weight 397.43
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Formula C20H29N3O9
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Color White to off-white
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SMILES
O=C(N1CCOCC1)NCCNCC(O)COC2=CC=C(O)C=C2.O=C(O)/C=C/C(O)=O
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Synonyms
Corwin hemifumarate; ICI 118587 hemifumarate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (251.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Ikram H, et al. Xamoterol in severe heart failure. Lancet. 1990 Aug 25;336(8713):517-8. [Content Brief]
[2]. Malta E, et al. The in vitro pharmacology of xamoterol (ICI 118,587). Br J Pharmacol. 1985;85(1):179-187. [Content Brief]
[3]. Kowalski MT, et al. Comparison of the effects of xamoterol and isoprenaline on rat cardiac beta-adrenoceptors: studies of function and regulation. Br J Pharmacol. 1990;99(1):27-30. [Content Brief]
[4]. Mehlsen J, et al. Xamoterol, a new selective beta-1-adrenoceptor partial agonist, in the treatment of postural hypotension. Acta Med Scand. 1986;219(2):173-177. [Content Brief]
[5]. Hashimoto T, et al. The cardiovascular effects of xamoterol, a beta 1-adrenoceptor partial agonist, in healthy volunteers at rest. Br J Clin Pharmacol. 1986;21(3):259-265. [Content Brief]
[6]. Löfdahl CG, et al. Effects of xamoterol (ICI 118,587) in asthmatic patients. Br J Clin Pharmacol. 1984;18(4):597-601. [Content Brief]
[7]. Jennings G, et al. Cardioselectivity, kinetics, hemodynamics, and metabolic effects of xamoterol. Clin Pharmacol Ther. 1984;35(5):594-603. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5162 mL | 12.5808 mL | 25.1617 mL | 62.9042 mL |
| 5 mM | 0.5032 mL | 2.5162 mL | 5.0323 mL | 12.5808 mL | |
| 10 mM | 0.2516 mL | 1.2581 mL | 2.5162 mL | 6.2904 mL | |
| 15 mM | 0.1677 mL | 0.8387 mL | 1.6774 mL | 4.1936 mL | |
| 20 mM | 0.1258 mL | 0.6290 mL | 1.2581 mL | 3.1452 mL | |
| 25 mM | 0.1006 mL | 0.5032 mL | 1.0065 mL | 2.5162 mL | |
| 30 mM | 0.0839 mL | 0.4194 mL | 0.8387 mL | 2.0968 mL | |
| 40 mM | 0.0629 mL | 0.3145 mL | 0.6290 mL | 1.5726 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2581 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4194 mL | 1.0484 mL | |
| 80 mM | 0.0315 mL | 0.1573 mL | 0.3145 mL | 0.7863 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6290 mL |
Xamoterol hemifumarate Related Classifications
HY-101327A Related Classifications
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- Xamoterol hemifumarate
- 73210-73-8
- Corwin hemifumarate
- ICI 118587 hemifumarate
- Adrenergic Receptor
- ischemic heart disease
- guinea-pig left atrial membranes
- heart failure
- progesterone-pretreated rat uterus
- β2-adrenoceptor
- rat atrial preparations
- cat left atria
- β1-adrenoceptor
- guinea pig
- postural hypotension
- Inhibitor
- inhibitor
- inhibit