2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. ML417

ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.

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ML417 Chemical Structure

ML417 Chemical Structure

CAS No. : 1386162-69-1

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25 mg USD 290 In-stock
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Based on 1 publication(s) in Google Scholar

ML417 Related Antibodies

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Description

ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons[1].

IC50 & TargetHY-P7488

D3 Receptor

38 nM (EC50)

In Vitro

ML417 exhibits a Ki for the D3R of 1.24 μM. ML417 is a full and potent agonist for multiple signaling pathways associated with D3R activation[1].
ML417 potently inhibits cAMP accumulation with an EC50 of 86 nM and an efficacy identical to that of dopamine. ML417 exhibits submicromolar affinity for only three of the targets, the β1-adrenergic, 5-HT2B serotoninergic, and σ-1 receptors. ML417 stimulates β-arrestin recruitment to the D3R-WT with an EC50 of 1.4 nM[1].
ML417 protects (0.005-5 μM; 24 hours) D3R-expressing dopaminergic neurons from 6-OHDA induced cell death[1].

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

ML417 Related Antibodies
In Vivo

In vivo pharmacokinetics experiments in mice (using 20 mg/kg; i.p.) reveals that ML417 is brain penetrant and exhibits a plasma half-life of 3.44 hours and a brain half-life of 4.23 hours. ML417 displays a plasma Tmax of 0.5 hours and Cmax of 6500 ng/ml, and a brain Tmax of 0.25 hours and Cmax of 28000 ng/ml[1].

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

Animal Model: 6-8 week old male C57BL/6 mice[1]
Dosage: 20 mg/kg
Administration: I.p. (Pharmacokinetic Analysis)
Result: Brain penetrant and exhibits a plasma half-life of 3.44 hours and a brain half-life of 4.23 hours. Displayed a plasma Tmax of 0.5 hours and Cmax of 6500 ng/ml, and a brain Tmax of 0.25 hours and Cmax of 28000 ng/ml.
Molecular Weight

379.45

Formula

C22H25N3O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C(N1)=CC2=C1C=CC=C2)N3CCN(CCOC4=CC=C(OC)C=C4)CC3
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: 

DMSO : 50 mg/mL (131.77 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 2.6354 mL 13.1770 mL 26.3539 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (13.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).
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.
Purity & Documentation
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
DMSO 1 mM 2.6354 mL 13.1770 mL 26.3539 mL 65.8848 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL 13.1770 mL
10 mM 0.2635 mL 1.3177 mL 2.6354 mL 6.5885 mL
15 mM 0.1757 mL 0.8785 mL 1.7569 mL 4.3923 mL
20 mM 0.1318 mL 0.6588 mL 1.3177 mL 3.2942 mL
25 mM 0.1054 mL 0.5271 mL 1.0542 mL 2.6354 mL
30 mM 0.0878 mL 0.4392 mL 0.8785 mL 2.1962 mL
40 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6471 mL
50 mM 0.0527 mL 0.2635 mL 0.5271 mL 1.3177 mL
60 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0981 mL
80 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8236 mL
100 mM 0.0264 mL 0.1318 mL 0.2635 mL 0.6588 mL
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ML417 Related Classifications

Help & FAQs
  • 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:

ML4171386162-69-1ML 417ML-417Dopamine Receptorβ-arrestintranslocationphosphorylationneuroprotectiondopaminergicneuronsInhibitorinhibitorinhibit

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