1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Carmoterol

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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Carmoterol

Carmoterol Chemical Structure

CAS No. : 147568-66-9

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Description

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)[1][2][3].

In Vitro

Carmoterol exhibits intrinsic activity comparable to Formoterol (HY-B0010A) in primary human bronchial smooth muscle cells, supporting a fast rate of cAMP accumulation[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Carmoterol exhibits rapid-onset and long-lasting bronchodilatory activity in guinea pigs and cats[1].
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.

Animal Model: Dunkin Hartley (male, 360-380 g)[3]
Dosage: 0.1 pmol, 0.3 pmol, 1 pmol, 3 pmol, 10 pmol, 30 pmol
Administration: intratracheal superfusion; 10 µL/min; 5 min
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.
Animal Model: Dunkin Hartley (male, 360-380 g, actively sensitized to ovalbumin)[3]
Dosage: 0.3 pmol, 1 pmol, 3 pmol, 10 pmol, 30 pmol
Administration: intratracheal superfusion; 10 µL/min; 5 min
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.
Molecular Weight

368.43

Formula

C21H24N2O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=C(C([C@@H](O)CN[C@H](C)CC3=CC=C(OC)C=C3)=CC=C2O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7142 mL 13.5711 mL 27.1422 mL
5 mM 0.5428 mL 2.7142 mL 5.4284 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. 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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Purity & Documentation
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. 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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Help & FAQs
  • 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.

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Carmoterol
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