Benzamil-hydrochloride-Benzylamiloride-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBenzamil hydrochlorideCat. No.: HY-B1546ACAS No.: 161804-20-2Synonyms: Benzylamiloride hydrochloride分式: CHClNO分量: 356.21作靶点: Sodium Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (280.73 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8073 mL 14.0367 mL 28.0733 mL5 mM 0.5615 mL 2.8073 mL 5.6147 mL10 mM 0.2807 mL 1.4037 mL 2.8073 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物

3、活性 Benzamil hydrochloride是钠通道（ENaC）的特异性阻断剂。IC50 & Target Sodium channel 1体外研究The specific ENaC blocker Benzamil hydrochloride adds to the luminal perfusate (106 M) significantlydecreases baseline Na+i by 19.2 mM (n=5) and almost completely inhibits the NaClL-dependent1/2 Master of Small Molecules 您边

4、的抑制剂师www.MedChemEincreasing in Na+i when coadministers with luminal AngII 2.体内研究 Intracerebroventricular injection of endothelin-1 (1 nmol) after intracerebroventricular preinjection of thevehicle of Benzamil hydrochloride markedly increases both mean arterial pressure and abdominalsympathetic nervo

5、us activity for 10 min. In SHRSP, intracerebroventricular infusion either of 1 or 10nmol/kg/day Benzamil hydrochloride decreases systolic blood pressure (4th day: F=6.131, 1 nmol/kg/day, P1.PROTOCOLCell Assay 2 Individual CCD segments are dissected from rabbit and mouse kidney.The measurements of Na

6、+i are usedas a reflection of Na+ transport across the apical membrane. EnaC-specific activity is assessed by applying106 M of the ENaC blocker Benzamil hydrochloride, a concentration that does not affect Na+:H+ exchange.Experiments are performed in the presence/absence of luminal Benzamil hydrochlo

7、ride or the Na:Hexchanger blocker HOE694 administers with/without the AT1 receptor blocker candesartan. Final DMSOconcentrations are below 0.1% 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal For the acute intracerebroventricular injection in a

8、nesthetized rats. A guide cannula is inserted into the rightAdministration 1 lateral cerebral ventricle, and Benzamil hydrochloride (0.1 nmol/kg, n=6; 1 nmol/kg, n=6; 10 nmol/kg,n=7) orvehicle (n=6) is injected into the right lateral ventricle through a cannula connected to a microsyringe 15 minbefo

9、re the start of intracerebroventricular infusion of hypertonic NaCl. Each injection consists of a volume of10 L deliver manually over a period of 30 s. To investigate the effects of Benzamil hydrochloride on thepressor response induced by intracerebroventricular injection of the pressor agent other

10、than hypertonicNaCl, endothelin-1, which has a potent pressor action in the brain of rats, is intracerebroventricularly injected(1 nmol/10 L) 15 min after the intracerebroventricular preinjection of Benzamil hydrochloride (10 nmol/kg,n=6) or the vehicle (n=6), and mean arterial pressure, heart rate,

11、 and abdominal sympathetic nerve firingsare recorded for 20 min. Catheters are implanted into both the femoral artery and vein of 12-wk-old male ratsanesthetized with urethan. Both catheters are filled with heparinized saline (50 U/mL). Fifteen minutes beforethe start of intracerebroventricular infu

12、sion of hypertonic NaCl, Benzamil hydrochloride (10 nmol/kg, n=6) orvehicle (10 L, n=6) is injected into a tube connects to the femoral venous catheter by directly inserting themicrosyringe, and 0.1 ml of isotonic saline solution is injected through the catheter to deliver the contents intothe venou

13、s circulation 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Nishimura M, et al. Benzamil blockade of brain Na+ channels averts Na(+)-induced hypertension in rats. Am J Physiol. 1998 Mar;274(3Pt 2):R635-44.2. Peti-Peterdi J, et al. Angiotensin II directly stimulates ENaC activity in the cortical collecting duct via AT(1) receptors. J Am Soc Nephrol.2002 May;13(5):1131-5.McePdfHeight2/2 Master of Small Molecules 您边的抑制