| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Carmoterol HCl targets the β2-adrenergic receptor, a G protein-coupled receptor that is primarily located in the airways. Activation of the β2-adrenergic receptor by Carmoterol HCl stimulates the production of cyclic AMP (cAMP) through adenylyl cyclase, leading to the relaxation of airway smooth muscle and bronchodilation. The compound's high selectivity for β2 over β1 receptors minimizes cardiovascular side effects.
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|---|---|
| ln Vitro |
In vitro, Carmoterol HCl is a highly potent and selective β2-adrenoceptor agonist with a pEC50 of 10.19. It has 53 times greater affinity for β2-adrenergic receptors than for β1-adrenergic receptors. Its activity is typically measured using receptor binding and functional assays. Functional assays measure the compound's ability to stimulate cAMP accumulation in cells expressing the β2-adrenergic receptor.
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| ln Vivo |
In vivo, Carmoterol HCl is a long-acting β2-adrenoceptor agonist (LABA) developed for the treatment of asthma and COPD. Like other LABAs, it works by binding to beta-2 adrenergic receptors in the airways, leading to relaxation of smooth muscle and bronchodilation. However, specific in vivo protocols and results are not detailed in standard product descriptions.
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| Enzyme Assay |
In vitro receptor binding assays for Carmoterol HCl measure its affinity for β2-adrenergic receptors. Membranes from cells expressing β2-adrenergic receptors are incubated with a radiolabeled β2 ligand and varying concentrations of Carmoterol HCl. The Ki is determined from competition binding curves. Selectivity is assessed by testing the compound against β1-adrenergic receptors.
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| Cell Assay |
In vitro cell-based assays for Carmoterol HCl are used to study its effects on β2-adrenergic receptor signaling. Cells expressing the β2-adrenergic receptor are treated with Carmoterol HCl, and the accumulation of cAMP is measured. The EC50 is determined from dose-response curves. These assays confirm the compound's potent and selective β2-adrenoceptor agonist activity.
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| Animal Protocol |
In vivo animal experiments for Carmoterol HCl are conducted in animal models of asthma and COPD. In a typical study, Carmoterol HCl is administered to animals, and its bronchodilatory effects are assessed by measuring airway resistance or lung function. The compound's ability to improve lung function is measured. These studies confirm the in vivo efficacy of Carmoterol HCl.
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| ADME/Pharmacokinetics |
Carmoterol HCl has a molecular weight of 404.89 g/mol and a molecular formula of C21H25ClN2O4. It has a CAS number of 137888-11-0. It is a solid compound. For storage, it is recommended to keep the powder at -20°C. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been characterized. Carmoterol HCl is administered by inhalation.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Carmoterol HCl is not provided in standard product descriptions. As a LABA, it may have side effects similar to other drugs in this class, including tachycardia, tremor, and headache. As with all research chemicals, standard laboratory safety precautions should be followed when handling Carmoterol HCl.
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| References |
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| Additional Infomation |
See also: Camoterol (notes moved to).
Carmoterol HCl is a research compound and is not approved for any clinical or therapeutic use. It is a highly potent, selective, and long-acting β2-adrenoceptor agonist (LABA). It has a pEC50 of 10.19 and has 53 times greater affinity for β2-adrenergic receptors than for β1-adrenergic receptors. Carmoterol HCl was developed for the treatment of asthma and COPD. It is a valuable research tool for studying β2-adrenergic receptor pharmacology. |
| Molecular Formula |
C21H25CLN2O4
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|---|---|
| Molecular Weight |
404.891
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| Exact Mass |
404.15
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| CAS # |
137888-11-0
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| Related CAS # |
Carmoterol;147568-66-9
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| PubChem CID |
63951
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
649.1ºC at 760mmHg
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| Flash Point |
346.4ºC
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| LogP |
3.689
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
518
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@H](CC1=CC=C(C=C1)OC)NC[C@@H](C2=CC=C(C3=C2C=CC(=N3)O)O)O.Cl
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| InChi Key |
SYCWERNQGSKYAG-QVRIGTRMSA-N
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| InChi Code |
InChI=1S/C21H24N2O4.ClH/c1-13(11-14-3-5-15(27-2)6-4-14)22-12-19(25)16-7-9-18(24)21-17(16)8-10-20(26)23-21;/h3-10,13,19,22,24-25H,11-12H2,1-2H3,(H,23,26);1H/t13-,19+;/m1./s1
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| Chemical Name |
8-hydroxy-5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]-1H-quinolin-2-one;hydrochloride
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| Synonyms |
CHF-4226 CHF4226TA2005 CHF 4226.01 TA-2005 hydrochlorideTA-2005 TA 2005 Carmoterol HCl Carmoterol hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~247.0 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (12.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (12.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 5 mg/mL (12.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4698 mL | 12.3490 mL | 24.6981 mL | |
| 5 mM | 0.4940 mL | 2.4698 mL | 4.9396 mL | |
| 10 mM | 0.2470 mL | 1.2349 mL | 2.4698 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-002094-46
Condition:Asthmatics patientsProducts are for research use only; We do not sell to patients
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