1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Almitrine mesylate

Almitrine mesylate (Synonyms: Almitrine bismesylate; Almitrine bismethanesulfonate; Almitrine dimesylate)

Cat. No.: HY-107319 Purity: 99.36%
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Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.

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

Almitrine mesylate Chemical Structure

Almitrine mesylate Chemical Structure

CAS No. : 29608-49-9

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Description

Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.

IC50 & Target

K+ channel[1]

In Vitro

Almitrine inhibits the activity of a high-conductance (152±13 pS), Ca2+-dependent K+ channel by decreasing its open probability. The IC50 value of the effect is 0.22 μM. The inhibitory effect of Almitrine on Ca2+-dependent K+ channels also is observed in GH3 cells. Almitrine at concentrations up to 10 μM does not affect whole-cell voltage-dependent K+, Ca2+, or Na+ currents in rat or rabbit cells. However, this concentration of Almitrine significantly inhibits the Ca2+-dependent component of K+ currents in rat chemoreceptor cells[1].

In Vivo

Almitrine acts via the peripheral arterial chemoreceptors raising carotid sinus nerve output and minute ventilation. Almitrine also has a pulmonary vascular action causing a dose-dependent constriction and dilatation. At low doses Almitrine enhances hypoxic pulmonary vasoconstriction and may improve the overall ventilation/perfusion ratio[2].

Molecular Weight

669.76

Formula

C₂₈H₃₇F₂N₇O₆S₂

CAS No.

29608-49-9

SMILES

C=CCNC1=NC(N(CC2)CCN2C(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)=NC(NCC=C)=N1.O=S(O)(C)=O.O=S(O)(C)=O

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 : 125 mg/mL (186.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4931 mL 7.4654 mL 14.9307 mL
5 mM 0.2986 mL 1.4931 mL 2.9861 mL
10 mM 0.1493 mL 0.7465 mL 1.4931 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Rats[2]
8-week-old male spf Wistar rats are used. Rats are anaesthetized with Thiobarbiturate inactin (BYK, 100 mg/kg, i.p.). The interaction of the ventilatory response to hypoxia and an intermittent (2 min on, 1 min break) low-dose (10 μg/kg per min) and high-dose (80 μg/kg per min) infusion of S9581 or Almitrine is tested in control and chronically hypoxic rats. S9581 or Almitrine is infused intravenously (100 μg/ mL). Inspired oxygen levels were controlled by passing oxygen-nitrogen mixtures across the tracheal port at a flow rate of 3-41 min-1[2].

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

References
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Almitrine mesylate
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