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Amiloride (MK-870)

Catalog No.GC31431

Amiloride (MK-870) (MK-870) is an inhibitor of both epithelial sodium channel (ENaC[1]) and urokinase-type plasminogen activator receptor (uTPA[2]).

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Amiloride (MK-870) Chemical Structure

Cas No.: 2609-46-3

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100mg
$41.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Podocytes

Preparation Method

Mature podocytes were treated with 50 mg/L lipopolysaccharide and 50 mg/L amiloride.

Reaction Conditions

50 mg/L amiloride;24h

Applications

Amiloride(MK-870) decreased uPAR expression (due to the presence of lipopolysaccharide) in podocytes.

Animal experiment [2]:

Animal models

C57BL/6 male mice

Preparation Method

Mice was intragastrically administered 10 mg/kg/d of amiloride 2 days ahead of the lipopolysaccharide injection.

Dosage form

10 mg/kg/d amiloride;3days;i. g.

Applications

Amiloride might inhibit uPAR expression in podocytes of transient proteinuria induced by lipopolysaccharid in the mouse model.

References:

[1]. Xu LB, Chi N, et,al.Amiloride, a urokinase-type plasminogen activator receptor (uTPA) inhibitor, reduces proteinurea in podocytes. Genet Mol Res. 2015 Aug 14;14(3):9518-29. doi: 10.4238/2015.August.14.15. PMID: 26345885.

Background

Amiloride (MK-870) is a selective T-type calcium channel blocker and an inhibitor of epithelial sodium channels (ENaC) and urokinase-type plasminogen activator receptor (uTPA), Ki=7 µM. It is also polycystin-2 (PC2;TRPP2) channel blocker[1-3].

Amiloride(50 mg/L;24h) decreased uPAR expression (due to the presence of lipopolysaccharide) in podocytes[4].

Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC50 (the concentration required to reach 50% inhibition of an ion channel) in the concentration range of 0.1 to 0.5 µM. Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger (NHE) with an IC50 as low as 3 µM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+][1]. Amiloride(0.1-1mM) together with Bumetanide completely blocked cell transition through G1 and entry into S-phase in BALB/c 3T3 cells [5].

Amiloride(10 mg/kg/d;3days;i.g.) might inhibit uPAR expression in podocytes of transient proteinuria induced by lipopolysaccharid in the mouse model[4]. In ApoE(-/-) mice, administration of amiloride(high-fat diets with 0.5% (w/w) amiloride;4 weeks) significantly suppressed LPS-accelerated atherosclerosis and LPS-induced increase of NHE1 activity, and reversed LPS-induced down-regulation of Bcl-2 expression[6]. Amiloride(2mg/kg/d;30days;i.p.) treatment in tumor-bearing mice(The CT26 and LLC cachexia cell models)distinctly alleviated muscle atrophy and relieved cachexia-related features without affecting tumor growth[7].

References:
[1]. Teiwes J, Toto RD. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17. doi: 10.1016/j.amjhyper.2006.05.022. PMID: 17198922.
[2]. Tang CM, Presser F, et,al. Amiloride selectively blocks the low threshold (T) calcium channel. Science. 1988 Apr 8;240(4849):213-5. doi: 10.1126/science.2451291. PMID: 2451291.
[3]. Giamarchi A, Feng S, et,al. A polycystin-2 (TRPP2) dimerization domain essential for the function of heteromeric polycystin complexes. EMBO J. 2010 Apr 7;29(7):1176-91. doi: 10.1038/emboj.2010.18. Epub 2010 Feb 18. PMID: 20168298; PMCID: PMC2857461.
[4]. Xu LB, Chi N, et,al.Amiloride, a urokinase-type plasminogen activator receptor (uTPA) inhibitor, reduces proteinurea in podocytes. Genet Mol Res. 2015 Aug 14;14(3):9518-29. doi: 10.4238/2015.August.14.15. PMID: 26345885.
[5]. Panet R, Snyder D, et,al. Amiloride added together with bumetanide completely blocks mouse 3T3-cell exit from G0/G1-phase and entry into S-phase. Biochem J. 1986 Nov 1;239(3):745-50. doi: 10.1042/bj2390745. PMID: 3548704; PMCID: PMC1147349.
[6]. Cui GM, Zhao YX, et,al.Amiloride attenuates lipopolysaccharide-accelerated atherosclerosis via inhibition of NHE1-dependent endothelial cell apoptosis. Acta Pharmacol Sin. 2013 Feb;34(2):231-8. doi: 10.1038/aps.2012.155. Epub 2012 Dec 31. PMID: 23274414; PMCID: PMC4011619.
[7]. Zhou L, Zhang T, et,al.Amiloride ameliorates muscle wasting in cancer cachexia through inhibiting tumor-derived exosome release. Skelet Muscle. 2021 Jul 6;11(1):17. doi: 10.1186/s13395-021-00274-5. PMID: 34229732; PMCID: PMC8258996.

Chemical Properties

Cas No. 2609-46-3 SDF
Canonical SMILES O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N
Formula C6H8ClN7O M.Wt 229.63
Solubility Soluble in DMSO 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 4.3548 mL 21.7742 mL 43.5483 mL
5 mM 0.871 mL 4.3548 mL 8.7097 mL
10 mM 0.4355 mL 2.1774 mL 4.3548 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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