Hexamethylene amiloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

HMA 是一种阿米洛利衍生物，可抑制 TRPA1 介导的钙信号 (IC50：35 μM)。它是 Na+/H+ 交换器 (NHE) 的抑制剂，各种 NHE 亚型的 Ki 为 0.013-2.4 μM。

HMA is an amiloride derivative, shown to inhibit TRPA1-mediated calcium signal (IC50: 35 μM). It is an inhibitor of the Na+/H+ exchanger (NHE), with Ki of 0.013-2.4 μM for various NHE isoforms. HMA also blocks ASIC3 channels by 51% at 20 μM.

5-(N,N-Hexamethylene)-amiloride inhibits human cardiac ion channels hERG (in CHO cells), Nav1.5 and Cav1.2 (in EHK293 cells) with of 3.3 μM, 30 μM, 8.3 μM, respectively, inelectrophysiology assays.5-(N,N-Hexamethylene)-amiloride (1 μM; 0-60 min; 37 ℃) exhibits microsomal stability, (1 μg/mL; 4.2 h; 37 ℃) shows mouse plasma stability and plasma protein binding, (20 μM; 4 h) displays Caco-2 cell permeability, cardiac ion channel activity.

5-(N,N-Hexamethylene)-amiloride (2.5 mg/kg; i.v.; single dose) shows short half-life and lowly oral bioavailability of 4.5%.In vivo pharmacokinetics in mice or rat model.Dosage: 2.5 mg/kg.Administration: Intravenous injection; single does; collected 10 min and 60 min after treatment.Note: B/P means blood-to-plasma partitioning ratio; female Balb/c mice (17-27 g, non-fasted); male SpragueDawley rats (238-325 g, overnight-fasted).

Hexamethylene amiloride | HMA

Cytoskeleton/Cell Adhesion Molecules

HSP

NHE exchangers| TRPA1| ASIC3| P2X7

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1428-95-1

311.77

C12H18ClN7O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (320.75 mM)

NC(=N)NC(=O)C1=C(N)N=C(N2CCCCCC2)C(Cl)=N1

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(-20℃)

With Ice Pack

≥ 2 years