Indacaterol-maleate-QAB149-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIndacaterol maleateCat. No.: HY-14299ACAS No.: 753498-25-8Synonyms: QAB149分式: CHNO分量: 508.56作靶點(diǎn): Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性

2、數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (196.63 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.9663 mL 9.8317 mL 19.6634 mL5 mM 0.3933 mL 1.9663 mL 3.9327 mL10 mM 0.1966 mL 0.9832 mL 1.9663 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)

3、結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.92 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.92 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% c

4、orn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (4.92 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Indacaterol (QAB149) 馬來酸鹽是超長效-腎上腺素受體激動(dòng)劑。IC50 & Target -adrenoceptor 1.體內(nèi)研究 Indacaterol (QAB149) inhibits cAMP production in Chinese hamster ovary cells stably transfected wit

5、hhuman 2 adrenoceptors with pEC50 of 8.06. Indacaterol (QAB149) inhibits electrically induced contractionon the electrically stimulated guinea pig trachea in a concentration-dependent manner with pEC50 of 8.23.Indacaterol induces a concentration-dependent inotropic effect with maximal efficacy of 75

6、% in the isolatedguinea pig left atrium 1. Indacaterol reverses the carbachol-induced contraction in a concentration-dependent manner with IC50 of 37 nM in human small airways. Indacaterol concentration dependentlyreverses the serotonin-induced contraction with IC50 of 10.5 nM in rat small airways.

7、Indacaterol has thehighest intrinsic efficacy of 53% in rat small airways and 73% in human small airways 2. Indacaterol(QAB149) (6.7 g/kg) inhibits 5-HT-induced bronchoconstriction with a maximal effect of 85% in theconscious guinea pig. Indacaterol (QAB149) (12.5 g/kg) dose-dependently inhibits met

8、hacholine-inducedbronchoconstriction with a maximal effect of 85% in the anesthetized rhesus monkey 1.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Neuroimmunol. 2019 Mar 28;332:37-48.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Battram, C., et al., In vitro and in vivo pharmacological characterization of

9、5-(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl-8-hydroxy-1H-quinolin-2-o ne (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action. J Pharmacol ExpTher, 2006. 317(2): p. 762-70.2. Sturton, R.G., et al., Pharmacological characterization of indacaterol, a novel once daily inhaled 2 adrenoceptor agonist, on smallairways in human and rat precision-cut lung slices. J Pharmacol Exp Ther, 2008. 324(1): p. 270-5.McePdfHeightCaution: Product has not been fully validated f