Almitrine mesylate (Almitrine bismesylate) |
| Catalog No.GC30891 |
El mesilato de almitrina (bismesilato de almitrina), un agonista de quimiorreceptores periféricos, inhibe selectivamente el canal K+ dependiente de Ca2+-.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 29608-49-9
Sample solution is provided at 25 µL, 10mM.
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Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.
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].
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].
[1]. López-López JR, et al. Effects of Almitrine bismesylate on the ionic currents of chemoreceptor cells from the carotid body. Mol Pharmacol. 1998 Feb;53(2):330-9. [2]. Bee D, et al. An analysis of the action of an analogue of Almitrine bismesylate in the rat model of hypoxic lung disease. Exp Physiol. 1992 Nov;77(6):819-28.
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Animal experiment: |
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]. |
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References: [1]. López-López JR, et al. Effects of Almitrine bismesylate on the ionic currents of chemoreceptor cells from the carotid body. Mol Pharmacol. 1998 Feb;53(2):330-9. |
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| Cas No. | 29608-49-9 | SDF | |
| Canonical 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 | ||
| Formula | C28H37F2N7O6S2 | M.Wt | 669.76 |
| Solubility | DMSO : 125 mg/mL (186.63 mM) | 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. |
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| 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 | 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 |
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Quality Control & SDS
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- Purity: >98.00%
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