| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
Normal guinea pigs were injected intravenously with graded doses of acetylcholine (10, 20, and 40 mg/kg) and histamine (5, 10, and 20 mg/kg). Alternatively, ovalbumin (5 mg/kg) was used to induce bronchoconstriction in animals that were already sensitized. ). The tracheal mucosa was infused with carboplatin (0.3 to 100 pmol) for five minutes prior to the challenge. With an ED50 of 16.7 pmol, carmoterol inhibits acetylcholine-induced bronchoconstriction in a dose-dependent manner[2].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: Male Dunkin Hartley guinea pig (body weight 360-380 g) [2]
Doses: 0.3 to 100 pmol. Route of Administration: By infusion (0.01 mL/min) into the tracheal mucosa for 5 minutes before challenge. Experimental Results: Dose-dependent inhibition of acetylcholine-induced bronchoconstriction. Very effective against reactions induced by histamine and ovalbumin, already effective at 1 pmol. |
| References |
[1]. Mario Cazzola, et al. β(2) -adrenoceptor agonists: current and future direction. Br J Pharmacol. 2011 May;163(1):4-17.
[2]. Giuseppe Rossoni, 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):250-7. |
| Molecular Formula |
C21H24N2O4
|
|---|---|
| Exact Mass |
368.173
|
| CAS # |
147568-66-9
|
| Related CAS # |
Carmoterol hydrochloride;137888-11-0
|
| PubChem CID |
63952
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
649.2±55.0 °C at 760 mmHg
|
| Flash Point |
346.4±31.5 °C
|
| Vapour Pressure |
0.0±2.0 mmHg at 25°C
|
| Index of Refraction |
1.616
|
| LogP |
1.9
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
27
|
| Complexity |
518
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
OC1=C2C(C=CC(=O)N2)=C(C(O)CNC(C)CC2C=CC(OC)=CC=2)C=C1
|
| InChi Key |
IHOXNOQMRZISPV-YJYMSZOUSA-N
|
| InChi Code |
InChI=1S/C21H24N2O4/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)/t13-,19+/m1/s1
|
| Chemical Name |
8-hydroxy-5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]-1H-quinolin-2-one
|
| Synonyms |
Carmoterol TA-2005 TA 2005 TA2005 CHF-4226 CHF4226CHF 4226
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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.) |
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.
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