Tenapanor,1234423-95-0

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YZ剂描述：

产品名称：Tenapanor

产品别名：AZD 1722; AZD1722; AZD-1722; RDX5791; RDX 5791; RDX-5791

英文别名：AZD 1722;AZD1722;AZD-1722;RDX5791;RDX 5791;RDX-5791

靶点：Sodium Channel

CAS：1234423-95-0

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.

溶解性：DMSO: 10 mM

体外研究：

Tenapanor exhibits human and rat NHE3 with IC50 values of 5 and 10 nM, respectively. Human intestinal transporters NHE1, NHE2, TGR5, ASBT, and Pit-1 and the sodium-dependent phosphate transporter NaPiIIb are not inhibited by tenapanor at concentrations up to 10 to 30 μM.

体内研究：Tenapanor plays a prominent role in sodium handling in the gastrointestinal tract and kidney. It acts exclusively in the gastrointestinal tract to inhibit sodium uptake when administered orally to rats. Average plasma Cmax values of tenapanor in rats and humans are less than 1 ng/mL with negligible area under the curve at doses of up to 30mg/kg in rats, 10mg/kg in dogs, and 900 mg in humans. Dose-dependent reductions in urinary sodium and increases in fecal sodium and luminal fluid mass are observed upon administering single doses of tenapanor to rats. Chronic administration of tenapanor to rats fed with standard chow (0.49% NaCl) causes a sustained reduction of urinary sodium and increase in fecal sodium.

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