Amiloride (MK-870) |
| Catalog No.GC31431 |
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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2609-46-3
Sample solution is provided at 25 µL, 10mM.
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.
| 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. | |
| 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 | DMSO : 100 mg/mL (435.48 mM; Need ultrasonic) | 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. | ||
| Prepare stock solution | |||
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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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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