| 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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| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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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