1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Amiloride hydrochloride

Amiloride hydrochloride (Synonyms: MK-870 hydrochloride)

Cat. No.: HY-B0285A Purity: >98.0%
Handling Instructions

Amiloride hydrochloride (MK-870 hydrochloride) is an epithelial sodium channel (ENaC) inhibitor and a competitive inhibitor of Urokinase-type plasminogen activator (uPA).

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Amiloride hydrochloride Chemical Structure

Amiloride hydrochloride Chemical Structure

CAS No. : 2016-88-8

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
500 mg USD 108 In-stock
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Other Forms of Amiloride hydrochloride:

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Description

Amiloride hydrochloride (MK-870 hydrochloride) is an epithelial sodium channel (ENaC) inhibitor and a competitive inhibitor of Urokinase-type plasminogen activator (uPA).

IC50 & Target

ENaC, uPA[1]

In Vitro

Amiloride blocks δβγ channels with an IC50 of 2.6 μM. 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[1]. 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)[2].

In Vivo

Amiloride (1 mg/kg/day) subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP) compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 90 mg/mL (338.23 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7581 mL 18.7906 mL 37.5813 mL
5 mM 0.7516 mL 3.7581 mL 7.5163 mL
10 mM 0.3758 mL 1.8791 mL 3.7581 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

266.09

Formula

C₆H₉Cl₂N₇O

CAS No.

2016-88-8

SMILES

O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N.Cl

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Amiloride hydrochloride
Cat. No.:
HY-B0285A
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Amiloride hydrochloride

Cat. No.: HY-B0285A