2. Neuronal Signaling
  3. Monoamine Oxidase
  4. Toloxatone

Toloxatone  (Synonyms: MD 69276)

製品番号: HY-14196 純度: 98.11%
COA 取扱説明書 Technical Support

Toloxatone (MD 69276) is a reversible, selective MAO-A inhibitor that can cross the blood-brain barrier. Toloxatone increases the levels of serotonin (5-HT) and norepinephrine in the brain. Toloxatone reduces the immobility time in the forced swimming test in mice, inhibits killing behavior in rats without causing sedation, and shows a correlation between its free plasma concentration and cerebrospinal fluid concentration. Toloxatone is widely used in research related to depression, depressive disorders and Parkinson's disease.

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Toloxatone

Toloxatone 構造式

CAS 番号 : 29218-27-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 在庫あり
Solution
10 mM * 1 mL in DMSO USD 72 在庫あり
Solid
5 mg $66 在庫あり
10 mg $110 在庫あり
25 mg $220 在庫あり
50 mg $365 在庫あり
100 mg $606 在庫あり
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500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

Toloxatone 関連抗体

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製品説明

Toloxatone (MD 69276) is a reversible, selective MAO-A inhibitor that can cross the blood-brain barrier. Toloxatone increases the levels of serotonin (5-HT) and norepinephrine in the brain. Toloxatone reduces the immobility time in the forced swimming test in mice, inhibits killing behavior in rats without causing sedation, and shows a correlation between its free plasma concentration and cerebrospinal fluid concentration. Toloxatone is widely used in research related to depression, depressive disorders and Parkinson's disease[1][2][3][4].

IC50 & Target

MAO-A

 

体外実験

Toloxatone (3-100 μM; 180 minutes) concentration-dependently decreases medium levels of DOPAL, DOPAC, DOPET, and DOPA and increases medium dopamine levels in rat pheochromocytoma PC12 cells, but requires relatively high concentrations to exert these effects[1].

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

Toloxatone 関連抗体
体内実験

Toloxatone (5-10 mg/kg; i.v.; single injection) exhibits dose-proportional pharmacokinetics over 5-10 mg/kg i.v. in anaesthetized male Fauve de Bourgogne rabbits, with a short terminal half-life (41.5-47.4 minutes for total drug), moderate volume of distribution (5.4-5.8 L), high total clearance (79-106 mL/min), weak plasma protein binding (28.1-32.2%), and rapid blood-brain barrier penetration resulting in CSF concentrations equivalent to unbound plasma concentrations[2].
Toloxatone (24.2-72.5 μmol/kg; i.p.; single dose) produces dose-dependent, sedation-independent inhibition of mouse killing behavior in spontaneous killer Wistar rats, with a maximum 82% inhibition observed at 72.5 μmol/kg (i.p.)[3].
Toloxatone (48.3 μmol/kg; i.p.; single dose) inhibits mouse killing behavior in PCPA (HY-B1368)-induced killer Wistar rats with 50% maximum inhibition at 48.3 μmol/kg (i.p.), with efficacy comparable to that seen in spontaneous killer rats[3].
Toloxatone (48.3 μmol/kg; i.p.; single dose) inhibits mouse killing behavior (MKB) in raphectomized killer Wistar rats with 58% maximum inhibition at 48.3 μmol/kg (i.p.), with efficacy comparable to that seen in spontaneous killer rats[3].
Toloxatone (256 mg/kg; i.p.; single acute dose; 30 minutes prior to test) produces a significant anti-immobility effect in the mouse forced swimming test model of depression, which is completely reversed by co-administration of diazepam 2 mg/kg[4].

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

Animal Model: Wistar rats (male, adult, 3-month-old, 250-350 g, spontaneous killer model via 1 month social isolation)[3]
Dosage: 24.2 μmol/kg; 48.3 μmol/kg; 72.5 μmol/kg
Administration: i.p.; single dose
Result: Achieved 60% maximum inhibition of mouse killing behavior (MKB), 45 min latency to inhibition, 65 min duration of inhibition (≥40% inhibition), and 18.8% efficacy at 24.2 μmol/kg.
Maintained unchanged locomotor activity relative to vehicle controls across 0-1, 1-2, and 2-3 hr intervals at 24.2 μmol/kg.
Achieved 63% maximum inhibition of MKB, 42 min latency to inhibition, 125 min duration of inhibition (≥40% inhibition), and 31.1% efficacy at 48.3 μmol/kg.
Maintained unchanged locomotor activity relative to vehicle controls across 0-1, 1-2, and 2-3 hr intervals at 48.3 μmol/kg.
Achieved 82% maximum inhibition of MKB, 54 min latency to inhibition, 140 min duration of inhibition (≥40% inhibition), and 32.2% efficacy at 72.5 μmol/kg.
Maintained unchanged locomotor activity relative to vehicle controls across 0-1, 1-2, and 2-3 hr intervals at 72.5 μmol/kg.
Animal Model: Wistar rats (male, adult, 3-month-old, 250-350 g, PCPA-induced killer model via 150 mg/kg PCPA i.p. for 2 consecutive days)[3]
Dosage: 48.3 μmol/kg
Administration: i.p.; single dose
Result: Achieved 50% maximum inhibition of mouse killing behavior (MKB), 75 min latency to inhibition, 72 min duration of inhibition (≥40% inhibition), and 21.7% efficacy.
Maintained unchanged locomotor activity relative to vehicle controls across 0-1, 1-2, and 2-3 hr intervals.
Showed no statistically significant differences in MKB inhibition parameters relative to spontaneous killer rats treated with the same dose of toloxatone.
Animal Model: Wistar rats (male, adult, 3-month-old, 250-350 g, raphectomized killer model via electrolytical destruction of dorsal and median raphe nuclei)[3]
Dosage: 48.3 μmol/kg
Administration: i.p.; single dose
Result: Achieved 58% maximum inhibition of mouse killing behavior (MKB), 41 min latency to inhibition, 103 min duration of inhibition (≥40% inhibition), and 25.0% efficacy.
Maintained unchanged locomotor activity relative to vehicle controls across 0-1, 1-2, and 2-3 hr intervals.
Showed no statistically significant differences in MKB inhibition parameters relative to spontaneous killer rats treated with the same dose of toloxatone.
分子量

207.23

分子式

C11H13NO3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC(N2C(OC(CO)C2)=O)=CC=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (603.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.8256 mL 24.1278 mL 48.2556 mL
5 mM 0.9651 mL 4.8256 mL 9.6511 mL
10 mM 0.4826 mL 2.4128 mL 4.8256 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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一般には略語で表示されます：C1V1 = C2V2

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Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (10.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (10.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 98.11%

COA (250 KB) LCMS (87 KB)

取扱説明書 (2659 KB)
参考文献

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8256 mL 24.1278 mL 48.2556 mL 120.6389 mL
5 mM 0.9651 mL 4.8256 mL 9.6511 mL 24.1278 mL
10 mM 0.4826 mL 2.4128 mL 4.8256 mL 12.0639 mL
15 mM 0.3217 mL 1.6085 mL 3.2170 mL 8.0426 mL
20 mM 0.2413 mL 1.2064 mL 2.4128 mL 6.0319 mL
25 mM 0.1930 mL 0.9651 mL 1.9302 mL 4.8256 mL
30 mM 0.1609 mL 0.8043 mL 1.6085 mL 4.0213 mL
40 mM 0.1206 mL 0.6032 mL 1.2064 mL 3.0160 mL
50 mM 0.0965 mL 0.4826 mL 0.9651 mL 2.4128 mL
60 mM 0.0804 mL 0.4021 mL 0.8043 mL 2.0106 mL
80 mM 0.0603 mL 0.3016 mL 0.6032 mL 1.5080 mL
100 mM 0.0483 mL 0.2413 mL 0.4826 mL 1.2064 mL
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Toloxatone Related Classifications

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

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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.

Keywords:

Toloxatone29218-27-7MD 69276MD69276MD-69276Monoamine OxidaseMAOnoradrenalinedepressionParkinson’s diseaseanaesthetized rabbitsmonoamine oxidase type A (MAO-A)rat pheochromocytoma PC12 cellsserotonin (5-HT)ratsmouse forced swimming testblood-brain barrierInhibitorinhibitorinhibit

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