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Mesaconitine is a nitric oxide synthase activator. Mesaconitine drives extracellular Na+ and Ca2+ influx into endothelial cells, increases intracellular Na+ and Ca2+ concentrations, and triggers nitric oxide release. Mesaconitine is applicable for pain-related research.

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

Mesaconitine

Mesaconitine Chemical Structure

CAS No. : 2752-64-9

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Based on 2 publication(s) in Google Scholar

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Description

Mesaconitine is a nitric oxide synthase activator. Mesaconitine drives extracellular Na+ and Ca2+ influx into endothelial cells, increases intracellular Na+ and Ca2+ concentrations, and triggers nitric oxide release. Mesaconitine is applicable for pain-related research[1][2][3].

In Vitro

Mesaconitine (30 μM) induces a sustained increase in [Ca2+]ᵢ in HUVECs with a net increase of 361 nM in normal buffer, which is dependent on extracellular Ca2+ and Na+, inhibited by the reverse-mode Na+/Ca2+ exchanger inhibitor KBR7943 and the nicotinic acetylcholine receptor inhibitor D-tubocurarine, and unaffected by the Na+/H+ exchanger inhibitor Cimetidine (HY-14289)[2].
Mesaconitine (100 μM) induces a small increase in [Na+]i in HUVECs, which is inhibited by the nicotinic acetylcholine receptor inhibitor D-tubocurarine[2].

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

In Vivo

Mesaconitine (20-60 μg/kg; s.c.; single dose) produces dose-dependent analgesia in the acetic acid-induced writhing model with an ED50 of 28 μg/kg (s.c.), an effect closely tied to the central noradrenergic system and not mediated via opiate receptors[3].
Mesaconitine (11 μg/kg; s.c.; single dose) produces dose-dependent central analgesia in the tail flick model with an ED50 of 11 μg/kg (s.c.), with activity modulated by central catecholaminergic agents; intracerebral administration (single dose) also induces dose-dependent analgesia that is more potent than morphine[3].
Mesaconitine (60 μg/kg; s.c.; single dose) modulates central catecholamine levels and turnover in rats, specifically accelerating norepinephrine depletion in select brain and spinal cord regions and dopamine depletion in the striatum when combined with α-methyl-p-tyrosine[3].

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

Animal Model: Std:ddY (male, 20-24 g)[3]
Dosage: 20 μg/kg; 60 μg/kg
Administration: s.c.; single dose (30 minutes prior to acetic acid injection)
Result: Exhibited dose-dependent analgesic activity with an ED50 of 28 μg/kg.
Reached maximum analgesic activity 40 minutes after s.c.
administration, with significant activity persisting for 4 hours at 20 μg/kg and 7 hours at 60 μg/kg.
Showed significantly reduced analgesia when co-administered with α-methyl-p-tyrosine, 6-hydroxydopamine, diethyldithiocarbamate, disulfiram, or reserpine.
Animal Model: Std:ddY (male, 20-24 g)[3]
Dosage: 11 μg/kg (s.c.); unspecified doses (i.c.)
Administration: s.c.; single dose (40 minutes prior to tail flick test); i.c.; single dose (30 minutes prior to tail flick test)
Result: Showed dose-dependent analgesic activity when administered intracerebrally, and was more potent than morphine.
Had an ED50 of 11 μg/kg (95% confidence limit: 4-28 μg/kg) when administered subcutaneously.
Reached maximum analgesic activity 40 minutes after s.c.
administration.
Showed significantly reduced analgesia when co-administered with α-methyl-p-tyrosine, 6-hydroxydopamine, or diethyldithiocarbamate.
Animal Model: Wistar (male, 200-220 g)[3]
Dosage: 60 μg/kg
Administration: s.c.; single dose
Result: Increased dopamine levels in the diencephalon, and norepinephrine and 5-hydroxytryptamine levels in the mesencephalon.
Accelerated the α-methyl-p-tyrosine-induced reduction of norepinephrine levels in the hippocampus, medulla oblongata plus pons, and spinal cord, and of dopamine levels in the striatum.
Molecular Weight

631.71

Formula

C33H45NO11

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CO[C@@H]1C2([C@@](C[C@@]3(O)[C@@H]4OC(C5=CC=CC=C5)=O)([H])[C@@]4([H])[C@](OC(C)=O)([C@@H](O)[C@@H]3OC)C6C2N(C)C7)[C@@]([C@H]6OC)([H])[C@@]7(COC)[C@H](O)C1

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

Ethanol : 4.62 mg/mL (7.31 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5830 mL 7.9150 mL 15.8300 mL
5 mM 0.3166 mL 1.5830 mL 3.1660 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation

Purity: 99.19%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol 1 mM 1.5830 mL 7.9150 mL 15.8300 mL 39.5751 mL
5 mM 0.3166 mL 1.5830 mL 3.1660 mL 7.9150 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mesaconitine
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HY-N0724
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