Carmoterol
Based on 1 Customer Validation
Carmoterol is a highly potent and selective long-acting β2-adrenergic receptor agonist with a pEC50 of 10.19. Carmoterol shows 53-fold higher affinity for β2-adrenergic receptors than for β1-adrenergic receptors. Carmoterol stimulates cyclic adenosine monophosphate accumulation, induces airway smooth muscle relaxation, inhibits bronchoconstriction, reduces thromboxane B2 release, and prolongs survival time. Carmoterol can be used in research related to asthma and chronic obstructive pulmonary disease (COPD).
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- Pureza: 99.36%
- No. CAS: 147568-66-9
- Fòrmula: C21H24N2O4
- Peso molecular:368.43
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Carmoterol exhibits rapid-onset and long-acting bronchodilatory effects, and its potency is superior to that of other long-acting β2-adrenergic receptor agonists in the guinea pig bronchoconstriction model[2].
Carmoterol (0.3-100 pmol; intratracheal instillation; 5 min) dose-dependently inhibits acetylcholine-induced bronchoconstriction in normal guinea pigs, with an ED50 of 16.7 pmol[3].
Carmoterol (0.1-30 pmol; intratracheal instillation; 5 min) potently and dose-dependently inhibits histamine-induced bronchoconstriction (ED50 = 2.7 pmol) and reduces histamine-induced TXB2 release (ED50 = 8.8 pmol) in normal guinea pigs[3].
Carmoterol (0.3-30 pmol; intratracheal instillation; 5 min) dose-dependently inhibits ovalbumin-induced allergic bronchoconstriction (ED50 = 9.5 pmol), reduces TXB2 release (ED50 = 11.8 pmol), and provides complete survival protection in sensitized guinea pigs at doses ≥ 3 pmol[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dunkin Hartley (male, 360-380 g)[3]
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Dosage:0.1 pmol, 0.3 pmol, 1 pmol, 3 pmol, 10 pmol, 30 pmol
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Administration:intratracheal superfusion; 10 µL/min; 5 min
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Result:Caused a dose-dependent inhibition of histamine-induced bronchoconstriction and reduction of plasma TXB2 levels.
Reached an ED50 value of 2.7 pmol for inhibition of ITP elevation.
Reached an ED50 value of 8.8 pmol for reduction of TXB2 release.
Reduced ITP elevation to 33.2% of maximal overflow and TXB2 levels to 4.06 ng/mL at 1 pmol.
Reduced ITP elevation to 24.9% of maximal overflow and TXB2 levels to 3.45 ng/mL at 3 pmol.
Reduced ITP elevation to 15.6% of maximal overflow and TXB2 levels to 2.77 ng/mL at 10 pmol.
Reduced ITP elevation to 7.8% of maximal overflow and TXB2 levels to 2.09 ng/mL at 30 pmol.
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Animal Model:Dunkin Hartley (male, 360-380 g, actively sensitized to ovalbumin)[3]
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Dosage:0.3 pmol, 1 pmol, 3 pmol, 10 pmol, 30 pmol
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Administration:intratracheal superfusion; 10 µL/min; 5 min
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Result:Caused a dose-dependent inhibition of ovalbumin-induced bronchoconstriction, reduction of plasma TXB2 levels, and prolongation of survival time.
Reached an ED50 value of 9.5 pmol for inhibition of ITP elevation.
Reached an ED50 value of 11.8 pmol for reduction of TXB2 release.
Reduced ITP elevation to 78.2% of maximal overflow at 1 pmol.
Reduced ITP elevation to 65.1% of maximal overflow and TXB2 levels to 14.4 ng/mL, and fully protected animals from death (survival time >60 min) at 3 pmol.
Reduced ITP elevation to 51.9% of maximal overflow and TXB2 levels to 11.8 ng/mL at 10 pmol.
Reduced ITP elevation to 33.1% of maximal overflow and TXB2 levels to 7.7 ng/mL at 30 pmol.
Chemical Information
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No. CAS 147568-66-9
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Appearance Solid
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Peso molecular 368.43
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Fòrmula C21H24N2O4
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Color White to off-white
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SMILES
O=C1NC2=C(C([C@@H](O)CN[C@H](C)CC3=CC=C(OC)C=C3)=CC=C2O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (271.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. 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)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Matera MG, et al. ultra-long-acting beta2-adrenoceptor agonists: an emerging therapeutic option for asthma and COPD?. Drugs. 2007;67(4):503-515. [Content Brief]
[2].
Cazzola M, et al. β(2) -adrenoceptor agonists: current and future direction. Br J Pharmacol. 2011 May;163(1):4-17.
[Content Brief]
[3]. Rossoni G, et al. Positive interaction of the novel beta2-agonist carmoterol and tiotropium bromide in the control of airway changes induced by different challenges in guinea-pigs. Pulm Pharmacol Ther. 2007;20(3):250-257. [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. 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 | 2.7142 mL | 13.5711 mL | 27.1422 mL | 67.8555 mL |
| 5 mM | 0.5428 mL | 2.7142 mL | 5.4284 mL | 13.5711 mL | |
| 10 mM | 0.2714 mL | 1.3571 mL | 2.7142 mL | 6.7855 mL | |
| 15 mM | 0.1809 mL | 0.9047 mL | 1.8095 mL | 4.5237 mL | |
| 20 mM | 0.1357 mL | 0.6786 mL | 1.3571 mL | 3.3928 mL | |
| 25 mM | 0.1086 mL | 0.5428 mL | 1.0857 mL | 2.7142 mL | |
| 30 mM | 0.0905 mL | 0.4524 mL | 0.9047 mL | 2.2618 mL | |
| 40 mM | 0.0679 mL | 0.3393 mL | 0.6786 mL | 1.6964 mL | |
| 50 mM | 0.0543 mL | 0.2714 mL | 0.5428 mL | 1.3571 mL | |
| 60 mM | 0.0452 mL | 0.2262 mL | 0.4524 mL | 1.1309 mL | |
| 80 mM | 0.0339 mL | 0.1696 mL | 0.3393 mL | 0.8482 mL | |
| 100 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6786 mL |
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