| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
δ Opioid Receptor/DOR
DPDPE TFA targets the δ-opioid receptor (DOR) as a selective agonist. It is a disulfide-containing cyclic opioid pentapeptide that selectively binds to the delta opioid receptor. DOR is a G protein-coupled receptor involved in pain modulation, seizure regulation, and other physiological processes. By selectively activating DOR, DPDPE TFA produces antinociceptive and anticonvulsant effects. Its selectivity for DOR over other opioid receptors makes it a valuable tool for studying DOR-specific signaling and function. |
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| ln Vitro |
In vitro, DPDPE TFA inhibits electrically stimulated contraction of mouse vas deferens with an EC50 of 5.2 nM. As a selective DOR agonist, it activates DOR-mediated signaling pathways. The compound's potent activity in the mouse vas deferens assay is a classic measure of opioid receptor agonist activity. It also possesses anticonvulsant properties. Detailed in vitro characterization data, including receptor binding assays and functional signaling studies, are available in the primary literature.
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| ln Vivo |
In vivo, DPDPE TFA is antinociceptive. As a selective DOR agonist with anticonvulsant properties, it has potential for in vivo investigations of pain modulation and seizure regulation. DOR agonists have been studied in animal models of pain and epilepsy. However, specific in vivo efficacy data and detailed animal model studies for this compound are limited in publicly available sources. Further research is needed to establish its full in vivo activity profile. The compound remains a research tool for DOR pharmacology.
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| Enzyme Assay |
For opioid receptor binding assays, membrane preparations from cells expressing recombinant DOR are incubated with radiolabeled ligands (e.g., [3H]-DPDPE or [3H]-naltrindole) and varying concentrations of DPDPE TFA. Non-specific binding is determined using excess unlabeled reference compounds (e.g., naltrindole). Following incubation at appropriate temperature (typically 25°C for 60-90 minutes), bound and free radioligands are separated by rapid filtration through glass fiber filters. Filters are washed and radioactivity counted by liquid scintillation. Ki values are calculated from competition curves. For functional assays, G protein activation is measured by [35S]-GTPγS binding.
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| Cell Assay |
For in vitro cellular assays, cell lines expressing DOR (e.g., CHO or HEK293 cells) are cultured in appropriate media under standard conditions (37°C, 5% CO2). DPDPE TFA is dissolved in DMSO or appropriate buffer and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. Receptor activation is assessed by measuring downstream signaling (e.g., cAMP inhibition, calcium flux, or ERK phosphorylation). For mouse vas deferens assays, tissue is mounted in organ baths and electrically stimulated, and inhibition of contraction is measured. Each concentration is tested in replicate with vehicle controls.
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| Animal Protocol |
For in vivo animal studies of DPDPE TFA, no specific published protocols are available. For general in vivo administration of DOR agonists, compounds are typically formulated in suitable vehicles and administered via intraperitoneal (i.p.) injection, subcutaneous (s.c.) injection, or intracerebroventricular (i.c.v.) injection. Dosing regimens vary by study objective. For pain models, nociceptive responses are measured. For anticonvulsant studies, seizure models may be used. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DPDPE TFA are characteristic of a cyclic peptide. The compound has a molecular weight of 645.79 (TFA salt), formula C30H39N5O7S2, and CAS number 172888-59-4. Purity: >98% (HPLC). Solubility: H2O 50 mg/mL (65.81 mM). Storage: -20°C. Stability: ≥2 years. As a peptide, it is typically administered parenterally and may have limited oral bioavailability and short half-life due to proteolytic degradation. Specific pharmacokinetic parameters are not extensively reported.
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| Toxicity/Toxicokinetics |
According to available safety information, DPDPE TFA is intended for research purposes only and is not for human use. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
A disulfide-bonded opioid pentapeptide that selectively binds to δ-opioid receptors has analgesic activity.
DPDPE TFA is a selective δ-opioid receptor (DOR) agonist peptide with anticonvulsant properties. It inhibits electrically stimulated contraction of mouse vas deferens (EC50 = 5.2 nM) and is antinociceptive in vivo. It has a molecular weight of 645.79 and formula C30H39N5O7S2. It is for research use only with no clinical development or regulatory approvals reported. |
| Molecular Formula |
C32H40F3N5O9S2
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|---|---|
| Molecular Weight |
759.813316345215
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| Exact Mass |
759.221
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| CAS # |
172888-59-4
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| Related CAS # |
DPDPE;88373-73-3
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| PubChem CID |
137700461
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
51
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| Complexity |
1130
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| Defined Atom Stereocenter Count |
4
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| SMILES |
S1C(C)(C)[C@H](C(NCC(NC(CC2C=CC=CC=2)C(N[C@@H](C(=O)O)C(C)(C)S1)=O)=O)=O)NC([C@H](CC1C=CC(=CC=1)O)N)=O.FC(C(=O)O)(F)F
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| InChi Key |
LUVILUYVBUMMRG-JZHXPYGKSA-N
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| InChi Code |
InChI=1S/C30H39N5O7S2.C2HF3O2/c1-29(2)23(34-25(38)20(31)14-18-10-12-19(36)13-11-18)27(40)32-16-22(37)33-21(15-17-8-6-5-7-9-17)26(39)35-24(28(41)42)30(3,4)44-43-29;3-2(4,5)1(6)7/h5-13,20-21,23-24,36H,14-16,31H2,1-4H3,(H,32,40)(H,33,37)(H,34,38)(H,35,39)(H,41,42);(H,6,7)/t20-,21-,23-,24-;/m0./s1
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| Chemical Name |
(4S,7S,13S)-13-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-7-benzyl-3,3,14,14-tetramethyl-6,9,12-trioxo-1,2-dithia-5,8,11-triazacyclotetradecane-4-carboxylic acid;2,2,2-trifluoroacetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 50 mg/mL (65.81 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3161 mL | 6.5806 mL | 13.1612 mL | |
| 5 mM | 0.2632 mL | 1.3161 mL | 2.6322 mL | |
| 10 mM | 0.1316 mL | 0.6581 mL | 1.3161 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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