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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.36%
- CAS 番号: 147568-66-9
- 分子式: C21H24N2O4
- 分子量:368.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Adrenergic Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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.
化学情報
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CAS 番号 147568-66-9
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性状 Solid
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分子量 368.43
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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 |
Carmoterol 関連分類
HY-12463A 関連分類
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