Almitrine-mesylate-Almitrine-bismesylate-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAlmitrine mesylateCat. No.: HY-107319CAS No.: 29608-49-9Synonyms: Almitrine bismesylate; Almitrine bismethanesulfonate; Almitrinedimesylate分式: CHFNOS分量: 669.76作靶點: Potassium Channel作通路: Membrane Transporter/Ion Channel儲存式: Powde

2、r -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (186.63 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.4931 mL 7.4654 mL 14.9307 mL5 mM 0.2986 mL 1.4931 mL 2.9861 mL10 mM 0.1493 mL 0.7465 mL 1.4931 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

3、液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Almitrine mesylate種外周 化學(xué)感受器的激動劑，選擇性抑制 Ca2+依賴性的 K+ 通道。IC50 & Target K+ channel 1體外研究Almitrine inhibits the activity of a high-conductance (15213 pS), Ca2+-dependent K+ channel by decreasing1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEits open probability. The IC50

4、value of the effect is 0.22 M. The inhibitory effect of Almitrine on Ca2+-dependent K+ channels also is observed in GH3 cells. Almitrine at concentrations up to 10 M does notaffect whole-cell voltage-dependent K+, Ca2+, or Na+ currents in rat or rabbit cells. However, thisconcentration of Almitrine

5、significantly inhibits the Ca2+-dependent component of K+ currents in ratchemoreceptor cells 1.體內(nèi)研究 Almitrine acts via the peripheral arterial chemoreceptors raising carotid sinus nerve output and minuteventilation. Almitrine also has a pulmonary vascular action causing a dose-dependent constriction

6、 anddilatation. At low doses Almitrine enhances hypoxic pulmonary vasoconstriction and may improve the overallventilation/perfusion ratio 2.PROTOCOLAnimal Rats 2Administration 2 8-week-old male spf Wistar rats are used. Rats are anaesthetized with Thiobarbiturate inactin (BYK, 100mg/kg, i.p.). The i

7、nteraction of the ventilatory response to hypoxia and an intermittent (2 min on, 1 min break)low-dose (10 g/kg per min) and high-dose (80 g/kg per min) infusion of S9581 or Almitrine is tested incontrol and chronically hypoxic rats. S9581 or Almitrine is infused intravenously (100 g/ mL). Inspiredox

8、ygen levels were controlled by passing oxygen-nitrogen mixtures across the tracheal port at a flow rate of3-41 min-1 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Lpez-Lpez JR, et al. Effects of Almitrine bismesylate on the ionic curren

9、ts of chemoreceptor cells from the carotid body. MolPharmacol. 1998 Feb;53(2):330-9.2. Bee D, et al. An analysis of the action of an analogue of Almitrine bismesylate in the rat model of hypoxic lung disease. Exp Physiol.1992 Nov;77(6):819-28.McePdfHeightCaution: Product has not been fully validated for medical