| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
κ Opioid Receptor/KOR
kappa-opioid receptor (KOR); also displays interaction with N-methyl-D-aspartate (NMDA) receptors. |
|---|---|
| ln Vitro |
Dynorphin A (1-13) exposure (33 μM) causes a discernible destruction of neuronal morphology at 16 hours, and a substantial loss of neuronal viability at 4 hours. Individual neurons' acute [Ca2+]i increases in response to dynorphin A (1–13) exposure are comparable to those observed following acute NMDA treatment.Over time, dynorphin A (1–13) (100 μM) exposure consistently results in a notable loss of neurons[1].
In vitro, porcine dynorphin A(1-13) binds to kappa-opioid receptors with high affinity and acts as a full agonist, activating G-protein signaling pathways that inhibit adenylyl cyclase and reduce cAMP production. The peptide shows selectivity for KOR over micro- and delta-opioid receptors. It has also been shown to interact with NMDA receptors, contributing to its complex pharmacological profile. The peptide has been used as a test compound in analytical applications including field asymmetric waveform ion mobility spectrometry coupled to mass spectrometry (FAIMS/IMS/MS). |
| ln Vivo |
Dynorphin A (1-13) exposure (33 μM) resulted in a significant loss of neuronal viability at 4 hours and a significant disruption of neuronal morphology at 16 hours. Exposure to dynorphin A (1-13) results in a dramatic increase in [Ca2+]i in single neurons, similar to the increase seen with acute NMDA treatment. Sustained exposure to dynorphin A (1-13) (100 μM) results in significant neuronal loss over time [1].
In vivo, porcine dynorphin A(1-13) exhibits antinociceptive effects in animal models at physiological concentrations. It is used to study the role of kappa-opioid receptors in pain modulation, stress responses, and neuropsychiatric disorders. The peptide is primarily a research tool and is not used clinically. |
| Enzyme Assay |
Receptor binding assays are performed using membrane preparations from cells expressing recombinant kappa-opioid receptors (e.g., CHO or HEK-293 cells) or from brain tissues (e.g., rat cortex). Membranes are incubated with radiolabeled [3H]-U69,593 or [3H]-dynorphin A (0.5-2 nM) and varying concentrations of unlabeled porcine dynorphin A(1-13) (0.01 nM-10 microM) in binding buffer (50 mM Tris-HCl, pH 7.4, containing 5 mM MgCl2, 1 mM EDTA, and 0.1% BSA) at 25degC for 60-90 minutes. Non-specific binding is determined in the presence of 10 microM unlabeled U69,593 or naloxone. Bound and free ligand are separated by rapid filtration through GF/B filters pre-soaked in 0.3% polyethyleneimine. Radioactivity is counted and Ki values are calculated from competitive binding curves.
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| Cell Assay |
Functional assays are performed in cells expressing recombinant kappa-opioid receptors. Cells are seeded in 96-well plates and pre-incubated with forskolin (1-5 microM) to stimulate cAMP production. Porcine dynorphin A(1-13) is added at concentrations ranging from 0.001 nM to 10 microM and incubated for 15-30 minutes at 37degC. Intracellular cAMP levels are measured using competitive ELISA or HTRF-based cAMP detection kits. Inhibition of cAMP accumulation is expressed as percentage of forskolin-stimulated control. EC₅0 values are calculated from dose-response curves. For GTPgammaS binding assays, membranes are incubated with GDP, GTPgamma[3⁵S], and varying concentrations of the peptide, and bound radioactivity is quantified. Calcium mobilization assays can also be performed using fluorescent calcium indicators.
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| Animal Protocol |
In vivo studies are performed in rodent models (mice or rats). Porcine dynorphin A(1-13) is administered via intracerebroventricular (ICV), intrathecal (IT), or intravenous routes at doses ranging from 0.1-10 nmol (ICV/IT) or 0.1-1 mg/kg (IV). Antinociceptive effects are evaluated using the tail-flick test, hot-plate test, or formalin test. Pain threshold is measured at multiple time points post-administration. The specificity of KOR-mediated effects is confirmed using KOR-selective antagonists (e.g., norbinaltorphimine, nor-BNI). For pharmacokinetic studies, blood and tissue samples are collected at various time points and peptide concentrations are measured by radioimmunoassay or LC-MS/MS.
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| ADME/Pharmacokinetics |
The peptide has molecular formula C₇₅H12₆N24O1₅ and molecular weight 1603.95. As a peptide, it has poor oral bioavailability and is administered parenterally. The half-life is short due to rapid proteolytic degradation. Stability can be enhanced by storage as a lyophilized powder at -20degC. The peptide sequence is Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for porcine dynorphin A(1-13). At pharmacological doses, the peptide is generally well-tolerated in animal studies. Potential adverse effects are related to KOR activation and may include dysphoria, sedation, or diuresis. The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
Porcine dynorphin A(1-13) is a potent endogenous kappa-opioid receptor agonist and research tool for studying opioid receptor pharmacology. It is a 13-amino acid fragment of the full-length dynorphin A peptide. The peptide is used to investigate KOR-mediated signaling, pain modulation, and neuropeptide-receptor interactions. It has also been employed as a test compound in analytical chemistry applications. Dynorphin A(1-13) is not an approved therapeutic agent; it is exclusively a research compound. The peptide is available as a research-grade product with high purity (≥97% HPLC).
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| Molecular Formula |
C75H126N24O15
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|---|---|
| Molecular Weight |
1603.95474
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| Exact Mass |
1602.983
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| CAS # |
72957-38-1
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| PubChem CID |
25075996
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.645
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| LogP |
-0.5
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
54
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| Heavy Atom Count |
114
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| Complexity |
3160
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| Defined Atom Stereocenter Count |
12
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| SMILES |
CCC(C(NC(C(NC(C(NC(C(NC(C(NC(CNC(CNC(C(N)CC1=CC=C(O)C=C1)=O)=O)=O)CC2=CC=CC=C2)=O)CC(C)C)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)C(NC(C(N3CCCC3C(NC(C(NC(C(NC(C(O)=O)CCCCN)=O)CC(C)C)=O)CCCCN)=O)=O)CCCNC(N)=N)=O)C
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| InChi Key |
OVVIBUHLQIYUEU-IWIISZHXSA-N
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| InChi Code |
InChI=1S/C75H126N24O15/c1-7-45(6)61(70(111)94-53(25-17-35-87-75(83)84)71(112)99-36-18-26-58(99)69(110)93-50(21-11-13-31-76)64(105)96-56(38-44(4)5)67(108)95-54(72(113)114)22-12-14-32-77)98-65(106)52(24-16-34-86-74(81)82)91-63(104)51(23-15-33-85-73(79)80)92-66(107)55(37-43(2)3)97-68(109)57(40-46-19-9-8-10-20-46)90-60(102)42-88-59(101)41-89-62(103)49(78)39-47-27-29-48(100)30-28-47/h8-10,19-20,27-30,43-45,49-58,61,100H,7,11-18,21-26,31-42,76-78H2,1-6H3,(H,88,101)(H,89,103)(H,90,102)(H,91,104)(H,92,107)(H,93,110)(H,94,111)(H,95,108)(H,96,105)(H,97,109)(H,98,106)(H,113,114)(H4,79,80,85)(H4,81,82,86)(H4,83,84,87)/t45-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,61-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]hexanoic acid
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| Synonyms |
Porcine dynorphin A(1-13); Dynorphin A Porcine Fragment 1-13
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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: ≥ 60 mg/mL (~37.4 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (62.35 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6235 mL | 3.1173 mL | 6.2346 mL | |
| 5 mM | 0.1247 mL | 0.6235 mL | 1.2469 mL | |
| 10 mM | 0.0623 mL | 0.3117 mL | 0.6235 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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