1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. nAChR
  3. Methyllycaconitine citrate

Methyllycaconitine citrate (Synonyms: MLA)

Cat. No.: HY-N2332A Purity: >98.0%
Handling Instructions

Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR).

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

Methyllycaconitine citrate Chemical Structure

Methyllycaconitine citrate Chemical Structure

CAS No. : 112825-05-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 115 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 270 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

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  • References

Description

Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR).

IC50 & Target

α7nAChR[1]

In Vitro

Pretreatment with 5 and 10 µM Methyllycaconitine citrate (MLA) inhibits the decreased cell viability induced by Aβ25-35. Cell viability does not decrease after exposure to Methyllycaconitine citrate (2.5, 5, 10, 20 µM). Aβ25-35 treatment increases LC3-II levels, which is inhibited by administration of Methyllycaconitine citrate. Methyllycaconitine citrate also inhibits Aβ-induced autophagosome accumulation in SH-SY5Y cells. Flow cytometry also demonstrates decreased MDC-labeled vacuoles with Methyllycaconitine citrate treatment[1].

In Vivo

Methyllycaconitine citrate (MLA) (6 mg/kg) given alone intraperitoneally does not cause climbing behavior when compare with the saline group. Pretreatment with Methyllycaconitine citrate significantly inhibits methamphetamine (METH)-induced climbing behavior, by about 50%. Methyllycaconitine citrate does not modify either basal locomotor activity or METH-induced hyperlocomotion. The METH-induced depletion of dopamine neuron terminals is attenuated in mice pretreated with Methyllycaconitine citrate (250±43 fmol/mg, n=7). A direct effect of Methyllycaconitine citrate on body temperature is ruled out because Methyllycaconitine citrate does not affect basal body temperature (37.0±0.5°C, n=5) or reduce the METH-induced hyperthermia (38.2±0.4°C, n=6, MLA+METH group, n.s. versus METH group)[1].

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 : 250 mg/mL (285.74 mM; Need ultrasonic and warming)

H2O : 2.18 mg/mL (2.49 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1430 mL 5.7148 mL 11.4296 mL
5 mM 0.2286 mL 1.1430 mL 2.2859 mL
10 mM 0.1143 mL 0.5715 mL 1.1430 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cells are plated in 96-well plates containing complete medium and cultured for 24 h. Then cells are treated with Methyllycaconitine citrate at the indicated concentrations for specified times. After drug treatment, cell viability is measured by MTT assay. Briefly, 10 µL of the MTT solution (5 mg/mL) is added to each well and incubated for 4 h at 37°C. After removing the supernatant, 100 µL DMSO is added into each well. The absorbance is measured at 570 nm with a microplate reader. All experiments are repeated 3 times[1].

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

Animal Administration
[2]

Adult male Swiss CD-1 mice are used in all experiments. They are housed at 22±1°C under a 12-h light/dark cycle with free access to food and drinking water. Climbing behavior is measured. Briefly, mice of 20 to 26 g are intraperitoneally administered saline (5 mL/kg) or Methyllycaconitine citrate (MLA) (6 mL/kg) at the beginning of the test. Twenty minutes later, the animals receive a single dose of saline or methamphetamine (METH) (1 mL/kg) subcutaneously and are placed individually, for habituation, into the experimental chamber consisting of a cylindrical cage with the wall made of plastic bars and covered with a lid. After a 20-min period of exploratory activity, stereotypy measurement is performed for a period of 30 min[2].

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

References
Molecular Weight

874.92

Formula

C₄₃H₅₈N₂O₁₇

CAS No.

112825-05-5

SMILES

CO[[email protected]@H]1C(C(N(CC)C2)C3(O)[[email protected]]4OC)([[email protected]@](C[[email protected]@]5([H])[[email protected]@H]6OC)([H])[[email protected]@]6([H])[[email protected]@]3(C[[email protected]@H]5OC)O)[[email protected]@]4([H])[[email protected]@]2(COC(C7=C(N(C8=O)C(C[[email protected]@H]8C)=O)C=CC=C7)=O)CC1.O=C(CC(C(O)=O)(O)CC(O)=O)O

Shipping

Room temperature in continental US; may vary elsewhere

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Methyllycaconitine citrate
Cat. No.:
HY-N2332A
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Methyllycaconitine citrate

Cat. No.: HY-N2332A