1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. DPDPE

DPDPE, an opioid peptide, is a selective δ-opioid receptor?(DOR) agonist?with anticonvulsant effects.

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DPDPE

DPDPE Chemical Structure

CAS No. : 88373-73-3

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Based on 1 publication(s) in Google Scholar

Other Forms of DPDPE:

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  • Biological Activity

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Description

DPDPE, an opioid peptide, is a selective δ-opioid receptor?(DOR) agonist?with anticonvulsant effects[1].

IC50 & Target

δ Opioid Receptor/DOR

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.12 nM
Compound: DPDPE
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
[PMID: 27096047]
CHO EC50
0.8 nM
Compound: DPDPE
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology measured over 30 mins by label free binding assay
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology measured over 30 mins by label free binding assay
[PMID: 25559207]
CHO EC50
1.3 nM
Compound: DPDPE
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
[PMID: 12672258]
CHO EC50
1.6 nM
Compound: DPDPE
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
[PMID: 16509592]
CHO EC50
1.6 nM
Compound: DPDPE, c[D-Pen2, D-Pen5]enkephalin
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
[PMID: 21128594]
CHO EC50
10 nM
Compound: DPDPE
Agonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
Agonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
[PMID: 27556704]
CHO EC50
13.2 nM
Compound: DPDPE
Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay
[PMID: 26525865]
CHO EC50
16 nM
Compound: DPDPE
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
[PMID: 18637671]
CHO EC50
2.05 nM
Compound: DPDPE
Agonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
Agonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
[PMID: 24103580]
CHO EC50
8.01 nM
Compound: DPDPE
Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay
Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay
[PMID: 26048798]
CHO EC50
9.29 nM
Compound: DPDPE
Agonist activity at human DOR expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human DOR expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 25248680]
CHO EC50
> 10000 nM
Compound: DPDPE
Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.
Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.
[PMID: 12672258]
CHO EC50
> 10000 nM
Compound: DPDPE
Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells
Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells
[PMID: 12672258]
CHO IC50
0.63 nM
Compound: DPDPE
Binding affinity against rat Opioid receptor delta 1 expressed in CHO cells determined by competitive inhibition of 1 nM [3H]DPDPE.
Binding affinity against rat Opioid receptor delta 1 expressed in CHO cells determined by competitive inhibition of 1 nM [3H]DPDPE.
[PMID: 9873480]
CHO IC50
1.3 nM
Compound: DPDPE
Displacement of [3H]DADLE from human recombinant delta-type 2 opioid receptor expressed in CHO cells
Displacement of [3H]DADLE from human recombinant delta-type 2 opioid receptor expressed in CHO cells
[PMID: 26988801]
CHO IC50
1.3 x 10-9 M
Compound: DPDPE
Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cells measured after 120 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
4 nM
Compound: DPDPE
Inhibitory activity against forskolin-stimulated cAMP production in chinese hamster ovary cells expressing Opioid receptor delta 1
Inhibitory activity against forskolin-stimulated cAMP production in chinese hamster ovary cells expressing Opioid receptor delta 1
[PMID: 9873480]
CHO-K1 EC50
6.34 nM
Compound: DPDPE
Agonist activity at human delta opioid receptor transfected in CHOK1 cells after 60 mins by [35S]GTPgammaS binding assay
Agonist activity at human delta opioid receptor transfected in CHOK1 cells after 60 mins by [35S]GTPgammaS binding assay
[PMID: 23659286]
HEK293 EC50
0.14 nM
Compound: DPDPE, c[D-Pen2,DPen5] enkephalin
Agonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
Agonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
[PMID: 21978284]
HEK293 EC50
0.557 nM
Compound: DPDPE
Agonist activity at Myc-tagged delta-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
Agonist activity at Myc-tagged delta-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
[PMID: 23477419]
HEK293 EC50
15 nM
Compound: 14, DPDPE
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
[PMID: 19683449]
HEK293 ED50
6.81 nM
Compound: DPDPE
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
[PMID: 22325949]
HEK293 IC50
0.0003 μM
Compound: DPDPE
Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
[PMID: 27776274]
HEK293 IC50
0.0009 μM
Compound: DPDPE
Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay
Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay
[PMID: 25087049]
HEK293 IC50
0.14 nM
Compound: DPDPE
Agonist activity at delta opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation
Agonist activity at delta opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation
[PMID: 20599386]
HEK293 IC50
1.12 nM
Compound: DPDPE
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK293 cells
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK293 cells
[PMID: 16989522]
HEK293 IC50
1.12 nM
Compound: DPDPE
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membranes
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membranes
[PMID: 17451272]
HEK293 IC50
1.2 nM
Compound: DPDPE
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membrane
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membrane
[PMID: 17388627]
HEK293 IC50
1.2 nM
Compound: DPDPE
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cells
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cells
[PMID: 18039010]
HEK293 IC50
1.2 nM
Compound: DPDPE
Displacement of [3H]deltorphin-2 from human delta opioid receptor expressed in HEK293 cell membrane
Displacement of [3H]deltorphin-2 from human delta opioid receptor expressed in HEK293 cell membrane
[PMID: 20426456]
HEK293 IC50
1.6 nM
Compound: DPDPE
Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method
Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method
[PMID: 27607020]
HEK293 IC50
1.6 nM
Compound: DPDPE
Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method
Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method
[PMID: 27607020]
LLC-PK1 IC50
> 50 μM
Compound: Enkephalin (DPDPE)
TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells
[PMID: 12699389]
LLC-PK1 IC50
> 50 μM
Compound: Enkephalin (DPDPE)
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells
[PMID: 12699389]
LLC-PK1 IC50
> 50 μM
Compound: Enkephalin (DPDPE)
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells
[PMID: 12699389]
LLC-PK1 IC50
> 50 μM
Compound: Enkephalin (dpdpe)
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
> 50 μM
Compound: Enkephalin (dpdpe)
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
> 50 μM
Compound: Enkephalin (dpdpe)
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
In Vivo

DPDPE (70 or 140 nM; i.c.v.; once) shows anticonvulsant effects in rats[1].
DPDPE (0.78–25 μg/mouse; i.c.v.; once) enhances bicuculline-induced convulsions in mouse[2].

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

Animal Model: Male Sprague-Dawley rats (225-275 g)[1]
Dosage: 70 or 140 nM followed by a 2 μl saline flush
Administration: Intracerebroventricular injection
Result: Resulted in a significant, dose-dependent increase in the convulsive threshold to flurothyl.
Animal Model: Male ddY mice weighing 20–30 g, pretreated with 1.5 mg/kg bicuculline (subcutaneous injection)[2].
Dosage: 0.78–25 μg/mouse, once
Administration: Intracerebroventricular injection
Result: Caused a dose-dependent increase in the proportion of mice exhibiting convulsions.
Molecular Weight

645.79

Formula

C30H39N5O7S2

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-{Pen}-Gly-Phe-{Pen} (Disulfide bridge:Pen2-Pen5)

Sequence Shortening

Y{Pen}GF{Pen} (Disulfide bridge:Pen2-Pen5)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 10 mg/mL (15.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5485 mL 7.7425 mL 15.4849 mL
5 mM 0.3097 mL 1.5485 mL 3.0970 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working 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).
Purity & Documentation

Purity: 99.61%

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 (sealed storage, away from moisture). 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
H2O 1 mM 1.5485 mL 7.7425 mL 15.4849 mL 38.7123 mL
5 mM 0.3097 mL 1.5485 mL 3.0970 mL 7.7425 mL
10 mM 0.1548 mL 0.7742 mL 1.5485 mL 3.8712 mL
15 mM 0.1032 mL 0.5162 mL 1.0323 mL 2.5808 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Product Name:
DPDPE
Cat. No.:
HY-P1334
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