2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Xamoterol hemifumarate

Xamoterol hemifumarate  (Synonyms: Corwin hemifumarate; ICI 118587 hemifumarate)

Cat. No.: HY-101327A Purity: 98.18%
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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.

Xamoterol hemifumarate

Xamoterol hemifumarate Chemical Structure

CAS No. : 73210-73-8

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Based on 1 publication(s) in Google Scholar

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Xamoterol hemifumarate Related Antibodies

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Description

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[1][2][3][4][5][6][7].

IC50 & Target[1]

β1 adrenoceptor

 

In Vitro

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 hemifumarate Related Antibodies
In Vivo

Xamoterol (0.1-33 μg/kg; i.v.; single bolus injection) hemifumarate acts as a β1-selective partial agonist in anaesthetised, catecholamine-depleted rats with an ED50 of 0.361 μg/kg[3].
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.

Animal Model: AS rats (200-300 g)[3]
Dosage: 600 μg/kg/h
Administration: s.c.; continuous infusion; 6 days
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.
Molecular Weight

397.43

Formula

C20H29N3O9
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCOCC1)NCCNCC(O)COC2=CC=C(O)C=C2.O=C(O)/C=C/C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5162 mL 12.5808 mL 25.1617 mL
5 mM 0.5032 mL 2.5162 mL 5.0323 mL
View the 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.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

SDS (419 KB)

COA (247 KB)

Handling Instructions (2659 KB)
References

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
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Xamoterol hemifumarate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Xamoterol hemifumarate73210-73-8Corwin hemifumarate ICI 118587 hemifumarateAdrenergic ReceptorBeta Receptorischemic heart diseaseguinea-pig left atrial membranesheart failureprogesterone-pretreated rat uterusβ2-adrenoceptorrat atrial preparationscat left atriaβ1-adrenoceptorguinea pigpostural hypotensionInhibitorinhibitorinhibit

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