DPDPE
Based on 2 publication(s) in Google Scholar
DPDPE, an opioid peptide, is a selective δ-opioid receptor?(DOR) agonist?with anticonvulsant effects.
For research use only. We do not sell to patients.
- Purity: 99.21%
- CAS No.: 88373-73-3
- Formula: C30H39N5O7S2
- Molecular Weight:645.79
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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)
Publications Citing Use of MedChemExpress (MCE) DPDPE
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Biological Activity
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δ Opioid Receptor/DOR |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>10000 nM
Compound: DPDPE
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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 | 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.
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[PMID: 12672258] |
| CHO | EC50 |
1.3 nM
Compound: DPDPE
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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
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[PMID: 16509592] |
| CHO | EC50 |
16 nM
Compound: DPDPE
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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
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[PMID: 18637671] |
| CHO | EC50 |
1.6 nM
Compound: DPDPE, c[D-Pen2, D-Pen5]enkephalin
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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
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[PMID: 21128594] |
| CHO | EC50 |
2.05 nM
Compound: DPDPE
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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 |
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 |
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 |
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
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[PMID: 26048798] |
| 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
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[PMID: 26525865] |
| 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 | 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 |
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 | IC50 |
1.3 nM
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 |
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 |
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 |
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 | 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 |
1.2 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 |
1.12 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 cells
Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cells
|
[PMID: 18039010] |
| 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 | 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 |
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 | 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 | 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 | 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 | 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 |
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] |
| 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 |
0.3 nM
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] |
| 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] |
| 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)
|
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] |
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.
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Animal Model:Male Sprague-Dawley rats (225-275 g)[1]
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Dosage:70 or 140 nM followed by a 2 μl saline flush
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Administration:Intracerebroventricular injection
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Result:Resulted in a significant, dose-dependent increase in the convulsive threshold to flurothyl.
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Animal Model:Male ddY mice weighing 20–30 g, pretreated with 1.5 mg/kg bicuculline (subcutaneous injection)[2].
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Dosage:0.78–25 μg/mouse, once
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Administration:Intracerebroventricular injection
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Result:Caused a dose-dependent increase in the proportion of mice exhibiting convulsions.
Chemical Information
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CAS No. 88373-73-3
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Appearance Solid
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Molecular Weight 645.79
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Formula C30H39N5O7S2
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Color White to off-white
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Sequence
Tyr-{Pen}-Gly-Phe-{Pen} (Disulfide bridge:Pen2-Pen5)
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Sequence Shortening
Y{Pen}GF{Pen} (Disulfide bridge:Pen2-Pen5)
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (2)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
H2O : 10 mg/mL (15.48 mM; Need ultrasonic)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. F C Tortella, et al. Anticonvulsant Effects of Mu (DAGO) and Delta (DPDPE) Enkephalins in Rats. Peptides [Content Brief]
[2]. Yajima Y, et al. Effects of differential modulation of mu-, delta- and kappa-opioid systems on bicuculline-induced convulsions in the mouse. Brain Res. 2000 Apr 17;862(1-2):120-6. [Content Brief]
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.