Tenapanor-AZD1722-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETenapanorCat. No.: HY-15991CAS No.: 1234423-95-0Synonyms: AZD1722; RDX5791分式: CHClNOS分量: 1145.05作靶点: Sodium Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体

2、外实验 DMSO : 50 mg/mL (43.67 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.18 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (2.18 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3

3、. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.18 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tenapanor钠氢离 (Na+/H+) 交换NHE3的抑制剂, 抑制和NHE3的IC50值分别为5和10 nM。IC50 & Target IC50: 5 nM (NHE3, human), 10 nM (NHE3, rat) 1体外研究 Tenapanor exhibits human and rat NHE3 with IC50 values of 5 and 10 nM, res

4、pectively. Human intestinaltransporters NHE1, NHE2, TGR5, ASBT, and Pit-1 and the sodium-dependent phosphate transporter NaPiIIbare not inhibited by tenapanor at concentrations up to 10 to 30 M 1.体内研究 Tenapanor plays a prominent role in sodium handling in the gastrointestinal tract and kidney. It ac

5、tsexclusively in the gastrointestinal tract to inhibit sodium uptake when administered orally to rats. Averageplasma Cmax values of tenapanor in rats and humans are less than 1 ng/mL with negligible area under thecurve at doses of up to 30mg/kg in rats, 10mg/kg in dogs, and 900 mg in humans. Dose-de

6、pendentreductions in urinary sodium and increases in fecal sodium and luminal fluid mass are observed uponadministering single doses of tenapanor to rats. Chronic administration of tenapanor to rats fed with standardchow (0.49% NaCl) causes a sustained reduction of urinary sodium and increase in fec

7、al sodium 1.PROTOCOLAnimal Rats: For urinary and fecal sodium assessments, 8-week-old Sprague-Dawley rats are randomized intoAdministration 1 groups before oral administration of vehicle or tenapanor (10ml/kg). After 16 to 24 hours, collected excretaare analyzed for electrolytes by ion chromatograph

8、y. In normal rats, tenapanor doses ranges from 0.1 to 10mg/kg. Higher doses within this range (1 to 10 mg/kg) are used to evaluate aldosterone levels and serumbicarbonate; lower doses (0.1 to 3 mg/kg) are used to evaluate urine electrolytes as well as other electrolytes1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Spencer AG, et al. Intestinal inhibition of the Na+/H+ exchanger 3 prevents cardiorenal damage in rats and inhibitsNa+ uptake inhumans.McePdfHeightCaution: Product has not been fully validated for medical a