Tulobuterol-hydrochloride _Adrenergic Receptor Agonist - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETulobuterol hydrochlorideCat. No.: HY-W011733CAS No.: 56776-01-3分式: CHClNO分量: 264.19作靶點: Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 D

2、MSO : 50 mg/mL (189.26 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.7852 mL 18.9258 mL 37.8515 mL5 mM 0.7570 mL 3.7852 mL 7.5703 mL10 mM 0.3785 mL 1.8926 mL 3.7852 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，

3、體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.46 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.46 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil

4、Solubility: 2.5 mg/mL (9.46 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Tulobuterol hydrochloride種 2-腎上腺素受體激動劑。IC50 & Target 2-adrenoceptor 1體外研究 Treatment of the cells with Tulobuterol (0.1 M) significantly decreases the viral titers of RV14 in thesupe

5、rnatants from 12 h after infection compared with the titers in the cells treated with vehicle (0.001%ethanol). Tulobuterol reduces RV14 release in a concentration-dependent manner. Pretreatment of the cellswith Tulobuterol reduces the viral titers of RV14 in the supernatants at concentrations of 0.1

6、 M or greater2.體內(nèi)研究 Tulobuterol, a sympathomimetic drug used as a transdermal patch, increases normal diaphragm musclestrength. In vivo effect of Tulobuterol is examined the on the contractility of diaphragm muscles preparedfrom mice treated with Endotoxin. In the in vivo treatment, E0 and E4 diaphr

7、agm muscles are analyzed at 0,12, and 24 h after transdermal Tulobuterol treatment. The force-frequency curves of E0 and E4 diaphragmmuscles at three time points are not significantly changed each other, indicating that Tulobuterol patchrestores the muscle contractility. Thus, diaphragm muscle contr

8、actility is maintained during 4 h of Endotoxinadministration with Tulobuterol patch for over 24 h 3.PROTOCOLCell Assay 2 To examine the effects of Tulobuterol, cultured human tracheal epithelial cells from the same donors aretreated with either Tulobuterol (0.1 M) or the vehicle (0.001% ethanol) fro

9、m 3 days (72 h) before RV14infection until the end of the experiments after RV14 infection 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Experiments are performed on 50 BALB/c mice weighing 21.70.2 g, which are divided

10、into 2 groups. In thetransdermal Tulobuterol treatment group, a small piece (44 mm2) of a 0.5 mg Tulobuterol patch sheet(1616 mm2) is affxed to the shaved back of each animal and covered with a small adhesive strip. Toexamine the effect of transdermal Tulobuterol treatment, the diaphragm muscles of

11、mice immediately afterE.coli Endotoxin (20 mg/kg) administration are dissected and measured for contractility at 0, 12, and 24 h(n=5 each) after patch affxation, termed T0E0, T12E0, and T24E0, respectively; to examine such effect 4 hafter E.coli Endotoxin (20 mg/kg) injection, the diaphragm muscles

12、of another group of mice are dissectedand measured for contractility at 0+4,12+4,and 24+4 h (n=5 each) after patch affxation,termed T0E4, T12E4,and T24E4, respectively.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ebihara S, et al. Cough

13、and transdermal long-acting beta2 agonist in Japan. Respir Med. 2008 Oct;102(10):1497; author reply 1498.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2. Yamaya M, et al. Tulobuterol inhibits rhinovirus infection in primary cultures of human tracheal epithelial cells. Physiol Rep. 2013Aug;1(3):e00041.3. Shindoh C, et al. Tulobuterol patch maintains diaphragm muscle contractility for over twenty-four hours in a mouse model of sepsis.Tohoku J Exp Med. 2009 Aug;218(4):271-