Amiloride HCl dihydrate (MK 870)

Alias: MK870; Amiloride Hydrochloride; MK-870; MK 870;Midamor; Midoride; Modamide.
Cat No.:V1652 Purity: ≥98%
Amiloride HCl dihydrate (MK870; MK-870; MK 870;Midamor; Midoride; Modamide),the hydrochloride salt and dihydrated form of amiloride, is a potent andselective epithelial sodium channel (ENaC) blocker that has been used since 1967 in the management of hypertension and congestive heart failure.
Amiloride HCl dihydrate (MK 870) Chemical Structure CAS No.: 17440-83-4
Product category: Sodium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
1g
25g
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Other Forms of Amiloride HCl dihydrate (MK 870):

  • Amiloride HCl (MK-870)
  • Amiloride (MK-870)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Amiloride HCl dihydrate (MK870; MK-870; MK 870; Midamor; Midoride; Modamide), the hydrochloride salt and dihydrated form of amiloride, is a potent and selective epithelial sodium channel (ENaC) blocker that has been used since 1967 in the management of hypertension and congestive heart failure.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Amiloride also induces the dephosphorylation of P13K (phosphatidylinositol 3-kinase) and PDK-1 (phosphoinositide-dependent kinase-1) kinases along with PTEN (phosphatase and tensin homolog deleted on chromosome 10) and PP1 alpha phosphatases. Amiloride inhibits phosphorylation of kinases and phosphatases by competing with ATP. Amiloride, which causes little or no cytotoxicity by itself, enhances TRAIL-induced apoptosis. Amiloride precludes the alkalinization and in parallel inhibit cellular proliferation. Amiloride directly inhibits autophosphorylation of the EGF receptor. Amiloride significantly enhances recovery to a maximum of 39%, 88%, and 78% for force, +dF/dt, and -dF/dt, respectively. Amiloride, a frequently used inhibitor of Na+/H+ exchange, rapidly inhibits phorbol ester-stimulated protein phosphorylation in vivo and protein kinase C-mediated phosphorylation in vitro, both with potency similar to that with which Amiloride inhibits Na+/H+ exchange. Amiloride blocks phorbol ester-induced adhesion of HL-60 cells (adhesion being a property indicative of the differentiated state), but dimethylamiloride (as well as ethylisopropylamiloride, another very potent amiloride analog) does not. Amiloride inhibits the ouabain-sensitive rate of oxygen consumption (QO2) of a suspension of rabbit intact proximal tubules in the presence of different concentrations of extracellular sodium.


Cell Assay: Amiloride blocks δβγ channels with an IC50 of 2.6 μM (58, 71, 75, 134, 148). The Ki of amiloride for δβγ ENaC is 26-fold that of αβγ channels (0.1 μM for αβγ ENaC). Amiloride blockade of δβγ ENaC is much more voltage dependent compared with the αβγ channel. The Ki of amiloride for δαβγ channels is 920 and 13.7 μM at -120 and +80 mV, respectively, which significantly differs from that of both αβγ and δβγ channels. 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+]. Amiloride is an even weaker inhibitor of the Na+/Ca2+ exchanger (NCX), with an IC50 of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na+ influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC).

ln Vivo
A strong inhibitor of epithelial sodium channels (ENaCs) is amiloride hydrochloride dihydrate. Within fifteen to thirty minutes after injection, amiloride is significantly concentrated in the plasma. When compared to the baseline readings (n = 7), a 2 mg/kg dose of amiloride hydrochloride dihydrate has no effect on blood pressure, heart rate, mesenteric vascular resistance, or hindquarters vascular resistance. Amiloride hydrochloride dihydrate causes very little change in heart rate (-10±6 bpm/min) and arterial pressure (-1±1 mmHg) over a 2-hour period when compared to baseline values. The c-Fos activation in the area postrema (AP) exhibits a dose-related response pattern, according to the results. Amiloride hydrochloride dihydrate, even at the lowest dose of 0.1 mg/kg, is statistically different from the control rats in terms of the number of c-Fos labeled neurons at the p<0.01 level[1].
Animal Protocol
1 mg/kg/day; subcutaneous
Rats
References
[1]. Miller RL, et al. Blockade of ENaCs by amiloride induces c-Fos activation of the area postrema. Brain Res. 2015 Mar 19;1601:40-51.
[2]. Xu LB, 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.
[3]. Giamarchi A, 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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C6H8CLN7O.HCL.2H2O
Molecular Weight
302.12
CAS #
17440-83-4
Related CAS #
Amiloride hydrochloride;2016-88-8;Amiloride;2609-46-3
SMILES
ClC1C(N([H])[H])=NC(=C(C(/N=C(\N([H])[H])/N([H])[H])=O)N=1)N([H])[H].Cl[H].O([H])[H].O([H])[H]
Chemical Name
3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride hydrate
Synonyms
MK870; Amiloride Hydrochloride; MK-870; MK 870;Midamor; Midoride; Modamide.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:60 mg/mL (198.6 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3099 mL 16.5497 mL 33.0994 mL
5 mM 0.6620 mL 3.3099 mL 6.6199 mL
10 mM 0.3310 mL 1.6550 mL 3.3099 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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