1. Membrane Transporter/Ion Channel
  2. Na+/Ca2+ Exchanger
    Sodium Channel
  3. Benzamil hydrochloride

Benzamil hydrochloride (Synonyms: Benzylamiloride hydrochloride)

Cat. No.: HY-B1546A Purity: 99.46%
Handling Instructions

Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na+/Ca2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca2+-activated currents, with an IC50 of 1.1 μM.

For research use only. We do not sell to patients.

Benzamil hydrochloride Chemical Structure

Benzamil hydrochloride Chemical Structure

CAS No. : 161804-20-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 79 In-stock
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50 mg USD 312 In-stock
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100 mg USD 552 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na+/Ca2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca2+-activated currents, with an IC50 of 1.1 μM[1][2][3].

In Vitro

Benzamil hydrochloride (Benzylamiloride hydrochloride) inhibits neuronal and heterologously expressed small conductance Ca2+-activated K2+ channels[4].

In Vivo

Benzamil hydrochloride (Benzylamiloride hydrochloride) (0.7 mg/kg/day; s.c.) treated stroke-prone spontaneously hypertensive rats (SHRSP) survived, on average, until 16.1 weeks of age in SHRSP rats[5].

Molecular Weight

356.21

Formula

C₁₃H₁₅Cl₂N₇O

CAS No.

161804-20-2

SMILES

O=C(C1=NC(Cl)=C(N)N=C1N)NC(NCC2=CC=CC=C2)=N.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

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 : ≥ 100 mg/mL (280.73 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8073 mL 14.0367 mL 28.0733 mL
5 mM 0.5615 mL 2.8073 mL 5.6147 mL
10 mM 0.2807 mL 1.4037 mL 2.8073 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Individual CCD segments are dissected from rabbit and mouse kidney.The measurements of [Na+]i are used as a reflection of Na+ transport across the apical membrane. EnaC-specific activity is assessed by applying 10−6 M of the ENaC blocker Benzamil hydrochloride, a concentration that does not affect Na+:H+ exchange. Experiments are performed in the presence/absence of luminal Benzamil hydrochloride or the Na:H exchanger blocker HOE694 administers with/without the AT1 receptor blocker candesartan. Final DMSO concentrations are below 0.1% [2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

For the acute intracerebroventricular injection in anesthetized rats. A guide cannula is inserted into the right lateral cerebral ventricle, and Benzamil hydrochloride (0.1 nmol/kg, n=6; 1 nmol/kg, n=6; 10 nmol/kg,n=7) or vehicle (n=6) is injected into the right lateral ventricle through a cannula connected to a microsyringe 15 min before the start of intracerebroventricular infusion of hypertonic NaCl. Each injection consists of a volume of 10 μL deliver manually over a period of 30 s. To investigate the effects of Benzamil hydrochloride on the pressor response induced by intracerebroventricular injection of the pressor agent other than hypertonic NaCl, endothelin-1, which has a potent pressor action in the brain of rats, is intracerebroventricularly injected (1 nmol/10 μL) 15 min after the intracerebroventricular preinjection of Benzamil hydrochloride (10 nmol/kg, n=6) or the vehicle (n=6), and mean arterial pressure, heart rate, and abdominal sympathetic nerve firings are recorded for 20 min. Catheters are implanted into both the femoral artery and vein of 12-wk-old male rats anesthetized with urethan. Both catheters are filled with heparinized saline (50 U/mL). Fifteen minutes before the start of intracerebroventricular infusion of hypertonic NaCl, Benzamil hydrochloride (10 nmol/kg, n=6) or vehicle (10 μL, n=6) is injected into a tube connects to the femoral venous catheter by directly inserting the microsyringe, and 0.1 ml of isotonic saline solution is injected through the catheter to deliver the contents into the venous circulation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

BenzamilBenzylamilorideNa+/Ca2+ ExchangerSodium ChannelNa channelsNa+ channelsneuronalchannelmyogenicvasoconstrictionpodocytesInhibitorinhibitorinhibit

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Benzamil hydrochloride
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