2. GPCR/G Protein Neuronal Signaling
  3. Melatonin Receptor
  4. 4-P-PDOT

4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).

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4-P-PDOT Chemical Structure

4-P-PDOT Chemical Structure

CAS No. : 134865-74-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 71 In-stock
Solution
10 mM * 1 mL in DMSO USD 71 In-stock
Solid
5 mg USD 65 In-stock
10 mg USD 110 In-stock
25 mg USD 226 In-stock
50 mg USD 376 In-stock
100 mg USD 625 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

4-P-PDOT Related Antibodies

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Description

4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity)[1][2][3][4].

IC50 & Target

MT2

 

In Vitro

In CHO-mt1 cells the amidotetraline 4-P-PDOT (10 mM) has no effect on forskolin-stimulated cyclic AMP levels, either alone, or in the presence of Melatonin. In contrast, in CHO-MT2 cells, 4-P-PDOT is an agonist, producing a concentration-dependent inhibition of forskolin stimulated cyclic AMP, with a pEC50 value of 8.72 and intrinsic activity of 0.86[1].

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

4-P-PDOT Related Antibodies

Cell Viability Assay[5]

Cell Line: HT-29 and HeLa cells.
Concentration: 50 µM
Incubation Time: 30 min
Result: Produced a negligible effect on cell viability induced by melatonin.
In Vivo

4-P-PDOT (0.5-1.0 mg/kg; intravenous injection; klotho mutant mice) treatment significantly reverses antioxidant effects mediated by Melatonin. And significantly reverses the changes in the levels of these GSH-related parameters. 4-P-PDOT treatment significantly reverses the memory function of Melatonin-treated klotho mutant mice. 4-P-PDOT also counteracts Melatonin-mediated attenuation in response to the decreases in phospho-ERK expression, Nrf2 nuclear translocation, Nrf2 DNA-binding activity, and GCL mRNA expression in the hippocampi of klotho mutant mice[2].

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

Animal Model: Klotho mutant mice treatment with Melatonin[2]
Dosage: 0.5 mg/kg or 1.0 mg/kg
Administration: Intravenous injection
Result: Significantly reversed antioxidant effects mediated by Melatonin. Significantly reversed the changes in the levels of these GSH-related parameters. Significantly reversed the memory function of Melatonin-treated klotho mutant mice.
Molecular Weight

279.38

Formula

C19H21NO
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

CCC(NC1CC2=C(C=CC=C2)C(C3=CC=CC=C3)C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (149.15 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 3.5794 mL 17.8968 mL 35.7935 mL
5 mM 0.7159 mL 3.5794 mL 7.1587 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 4.17 mg/mL (14.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 4.17 mg/mL (14.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.17 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 (41.7 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

Purity: 99.80%

SDS (392 KB)

COA (250 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. 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 3.5794 mL 17.8968 mL 35.7935 mL 89.4839 mL
5 mM 0.7159 mL 3.5794 mL 7.1587 mL 17.8968 mL
10 mM 0.3579 mL 1.7897 mL 3.5794 mL 8.9484 mL
15 mM 0.2386 mL 1.1931 mL 2.3862 mL 5.9656 mL
20 mM 0.1790 mL 0.8948 mL 1.7897 mL 4.4742 mL
25 mM 0.1432 mL 0.7159 mL 1.4317 mL 3.5794 mL
30 mM 0.1193 mL 0.5966 mL 1.1931 mL 2.9828 mL
40 mM 0.0895 mL 0.4474 mL 0.8948 mL 2.2371 mL
50 mM 0.0716 mL 0.3579 mL 0.7159 mL 1.7897 mL
60 mM 0.0597 mL 0.2983 mL 0.5966 mL 1.4914 mL
80 mM 0.0447 mL 0.2237 mL 0.4474 mL 1.1185 mL
100 mM 0.0358 mL 0.1790 mL 0.3579 mL 0.8948 mL
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4-P-PDOT 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:

4-P-PDOT134865-74-0Melatonin ReceptorNrf2 ERKoxidativedamageGSHGSSGMT2memoryMelatoninInhibitorinhibitorinhibit

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