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5-(N,N-dimethyl)-Amiloride (hydrochloride) (Synonyms: DMA,L-591,605,MK-685)

Catalog No.GC10898

NHE1, NHE2, and NHE3 inhibitor

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5-(N,N-dimethyl)-Amiloride (hydrochloride) Chemical Structure

Cas No.: 2235-97-4

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5mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

5-(N, N-dimethyl)-Amiloride (hydrochloride), a derivative of amiloride, is an inhibitor of NHE1, NHE2, and NHE3.

The Na+/H+ exchanger (NHE) is a protein that has been involved in intracellular pH homeostasis of many mammalian cell types. NHE is involved in regulating intracellular pH and cell volume by extruding protons from, and taking up sodium ions into cells [1].

5-(N, N-dimethyl)-Amiloride (DMA) inhibited NHE1, NHE2, and NHE3 with Ki values of 0.02, 0.25, and 14 μM, respectively. DMA showed little or no effects on NHE4, NHE5, and NHE7 [1]. DMA could effectively protect the right ventricular wall against ischemia-reperfusion dysfunction in the presence or absence of ouabain [2]. DMA protected against severe reperfusion-induced cardiac contractile dysfunction, appeared to act via a normalization of tissue sodium levels [2]. DMA (0.2 mM) completely inhibited pHi recovery after cell acidification and blocked EGF-induced cytoprotection against acid [3].

In primary rat hepatocyte cultures and rat liver plasma membranes, DMA increased steady-state Na+ content and inhibited ouabain-sensitive 86Rb+ uptake in a reversible, concentration-dependent, ouabain-like manner, with estimated IC50 of 5.2×10-4 M. DMA also inhibited ouabain-sensitive ATP hydrolysis in rat liver plasma membranes with IC50 value of 2.2 ×10-3 M. DMA (10-3 M) decreased the uptake into hepatocytes of alanine by 61% [4].

References:
[1] Masereel B, Pochet L, Laeckmann D.  An overview of inhibitors of Na+/H+ exchanger[J]. European journal of medicinal chemistry, 2003, 38(6): 547-554.
[2] Meng H, Pierce G N.  Involvement of sodium in the protective effect of 5-(N, N-dimethyl)-amiloride on ischemia-reperfusion injury in isolated rat ventricular wall[J]. Journal of Pharmacology and Experimental Therapeutics, 1991, 256(3): 1094-1100.
[3] Fujiwara Y, Higuchi K, Takashima T, et al.  Roles of epidermal growth factor and Na+/H+ exchanger-1 in esophageal epithelial defense against acid-induced injury[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2006, 290(4): G665-G673.
[4] Renner E L, Lake J R, Cragoe E J, et al.  Amiloride and amiloride analogs inhibit Na+/K+-transporting ATPase and Na+-coupled alanine transport in rat hepatocytes[J]. Biochimica et Biophysica Acta (BBA)-Biomembranes, 1988, 938(3): 386-394.

Chemical Properties

Cas No. 2235-97-4 SDF
Synonyms DMA,L-591,605,MK-685
Chemical Name 3-amino-N-(aminoiminomethyl)-6-chloro-5-(dimethylamino)-2-pyrazinecarboxamide, monohydrochloride
Canonical SMILES CN(C)C1=NC(N)=C(C(NC(N)=N)=O)N=C1Cl.Cl
Formula C8H12ClN7O • HCl M.Wt 294.1
Solubility ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.4002 mL 17.001 mL 34.002 mL
5 mM 0.68 mL 3.4002 mL 6.8004 mL
10 mM 0.34 mL 1.7001 mL 3.4002 mL
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