![Deltorphin 2 TFA ([D-Ala2]-Deltorphin II TFA)](/upload/1124/V77093.png)
| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
δ Opioid Receptor/DOR
Deltorphin 2 TFA specifically targets the delta-opioid receptor (delta-opioid receptor or DOR). It acts as a potent and highly selective full agonist. While the parent deltorphin from frogs has a Ki of approximately 1-2 nM for the delta-receptor with a selectivity of thousands-fold over the micro-receptor, [D-Ala2]-Deltorphin II demonstrates an even higher selectivity for delta-receptors. The binding affinity for the delta-opioid receptor is in the low nanomolar range with a Ki value of approximately 0.4-2.0 nM. It shows very weak binding to micro- and kappa-opioid receptors (micro: IC50 > 1000 nM; kappa: IC50 > 1000 nM). |
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| ln Vitro |
Deltorphin 2 ([D-Ala2]-Deltorphin II) is an amphibian heptapeptide with a high affinity and specificity for the delta-opioid receptor that is enzymatically stable. The most effective natural agonist for the delta opioid receptor is dextorphin 2[1].
In vitro, Deltorphin 2 ([D-Ala2]-Deltorphin II) is described as the most selective natural delta-opioid receptor agonist. It potently inhibits adenylate cyclase activity (via Gi/o protein coupling) and stimulates [35S]GTPgammaS binding in membranes expressing the delta-opioid receptor. The compound also induces receptor internalization in cell lines. It is an enzymatically stable heptapeptide, demonstrating resistance to proteolytic degradation compared to native enkephalins, a property that makes it superior for many ex vivo experimental setups where prolonged receptor stimulation is required. |
| ln Vivo |
In vivo, Deltorphin 2 TFA produces antinociceptive (pain-relieving) effects primarily through activation of the delta-opioid receptor when administered supraspinally (intracerebroventricular, ICV) or intrathecally (IT) in rodent models. It does not produce the typical morphine-like side effects such as respiratory depression, physical dependence, or significant gastrointestinal transit inhibition (constipation). In animal models of depression and anxiety, delta opioid receptor agonists, including Deltorphin 2, exhibit antidepressant-like and anxiolytic-like effects. Its enzymatic stability contributes to a more prolonged duration of action in vivo compared to other native peptide agonists.
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| Enzyme Assay |
Delta-opioid receptor binding assays are performed in vitro using radioligand competition binding. Protocols typically use membranes prepared from CHO or HEK-293 cells stably expressing the human or rodent delta-opioid receptor. The radioligand is typically [3H]-Naltrindole (a delta-selective antagonist) or [3H]-Deltorphin II. Membranes (10-50 microg protein) are incubated with a fixed concentration of radioligand (e.g., 0.5-2 nM) and increasing concentrations of Deltorphin 2 TFA (0.1 pM - 10 microM) in a total volume of 250-500 microL of 50 mM Tris-HCl buffer (pH 7.4) containing 100 mM NaCl and 10 microM GTP for 60-90 min at 25degC. Non-specific binding is defined with 10 microM unlabeled Naltrondine. Bound radioactivity is separated by rapid filtration through GF/B filters and counted. Ki values are calculated from IC50 using the Cheng-Prusoff equation.
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| Cell Assay |
Functional activity can be assessed via [35S]GTPgammaS binding assays or cAMP accumulation assays in delta-opioid receptor-expressing cells. For [35S]GTPgammaS assays, CHO cells expressing DOR are harvested and membrane homogenates are prepared. The membranes are resuspended in assay buffer (20 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM MgCl2, 1 microM GDP). For each reaction, 5-20 microg of membranes are incubated with 0.1 nM [35S]GTPgammaS, various concentrations of Deltorphin 2 TFA (0.1 pM - 10 microM), and 30 microM GDP in a final volume of 500 microL for 60 min at 30degC. The reaction is terminated by filtration through GF/B filters. Bound radioactivity is measured by scintillation counting. For cAMP inhibition assays, cells are pre-incubated with 100 microM IBMX for 10 min, then stimulated with 1-10 microM forskolin to elevate cAMP levels, with or without Deltorphin 2 TFA for 15 min. Cyclic AMP levels are measured using a competitive EIA or HTRF kit. The EC50 for inhibition of adenylyl cyclase is determined.
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| Animal Protocol |
For in vivo antinociception studies, adult male Sprague-Dawley rats (250-300 g) or C57BL/6J mice (20-25 g) are used. The tail-flick or hot-plate test is the standard analgesic assay. Baseline latency (sec) is recorded. Deltorphin 2 TFA is dissolved in sterile artificial cerebrospinal fluid (aCSF) or 0.9% saline. For central administration: Intracerebroventricular (ICV) injection is given via a pre-implanted guide cannula (coordinates: -0.5 mm AP, +/-1.0 mm ML, 2.5 mm DV from bregma). Doses: 0.1-30 nmol/rat or 0.01-3 nmol/mouse. For intrathecal (IT) injection, the lumbar puncture technique is used (L5-L6 intervertebral space). Doses: 0.1-100 nmol/rat. Following injection, tail-flick latency is measured every 15-30 min for up to 90-120 min. Maximum antinociceptive effect (%MPE) is calculated as [(test latency - baseline latency) / (cut-off time - baseline latency)] × 100. Typically, a cut-off time of 10-15 s is used to prevent tissue damage.
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| ADME/Pharmacokinetics |
No clinical pharmacokinetic (PK) data available for the research compound Deltorphin 2 TFA in humans. Based on animal studies, when administered directly into the central nervous system (i.c.v. or i.t.), the peptide exhibits a short duration of action (typically 30-90 min), consistent with its half-life in the cerebrospinal fluid (CSF) of ~15-30 min. Systemic administration is not effective due to poor blood-brain barrier penetration. The TFA counterion improves solubility and handling; the free peptide is soluble in water and acidic solutions (pH < 6). Enzymatic stability is conferred by the D-Ala2 residue, but the peptide is still subject to some proteolytic cleavage.
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| Toxicity/Toxicokinetics |
The acute toxicity of Deltorphin 2 TFA is low in experimental animals at doses producing antinociception. The therapeutic window (TD50/ED50) in rodents is estimated to be >100, indicating a high margin of safety for centrally-administered delta-agonists. No significant motor impairment, respiratory depression, or gastrointestinal side effects are reported at antinociceptive doses. At very high doses (100-fold higher than the ED50), transient sedation or mild ataxia may occur, but this is reversible. There is no evidence of physical dependence or withdrawal signs upon cessation of treatment, a significant advantage over mu-opioid analgesics. No organ-specific toxicity (hepatotoxicity, nephrotoxicity) has been described for this research peptide in published literature.
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| References | |
| Additional Infomation |
Deltorphin 2 TFA (also known as [D-Ala2]-Deltorphin II) is the TFA salt of a peptide hormone analog. Its chemical sequence is Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2. It is a member of the deltorphin family, which are naturally occurring heptapeptides isolated from the skin of the South American frog Phyllomedusa bicolor. The substitution of L-Ala2 with D-Ala2 in the synthetic analog enhances both potency and metabolic stability. Unlike morphine, which acts on micro-receptors, Deltorphin 2 provides analgesia without the common side effects of respiratory depression, addiction potential, and constipation. This profile makes it a lead tool compound for developing non-addictive pain therapies. Deltorphin 2 TFA is for research use only and is not for human therapeutic, diagnostic, or clinical use.
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| Molecular Formula |
C40H55F3N8O12
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| Molecular Weight |
896.91
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| Related CAS # |
Deltorphin 2;122752-16-3
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| Appearance |
White to off-white solid powder
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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) |
DMSO :~50 mg/mL (~55.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1149 mL | 5.5747 mL | 11.1494 mL | |
| 5 mM | 0.2230 mL | 1.1149 mL | 2.2299 mL | |
| 10 mM | 0.1115 mL | 0.5575 mL | 1.1149 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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