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

4-P-PDOT 

Cat. No.: HY-100609 Purity: 99.45%
COA Handling Instructions

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).

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

4-P-PDOT Chemical Structure

4-P-PDOT Chemical Structure

CAS No. : 134865-74-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 99 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

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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 receptor[1]
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].

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

Cell Viability Assay[5]

Cell Line: HT-29 and HeLa cells.
Concentration: 30 min.
Incubation Time: 50 µM.
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].

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

Appearance

Solid

Formula

C19H21NO
CAS No.
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)

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
10 mM 0.3579 mL 1.7897 mL 3.5794 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.45%

COA (250 KB) HNMR (218 KB) RP-HPLC (194 KB) MS (105 KB)

Handling Instructions (2659 KB)
References
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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.

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Keywords:

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

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