| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
Dynorphin (1-8) targets the kappa opioid receptor (KOR), a G protein-coupled receptor that is part of the endogenous opioid system. It is the most likely natural ligand for the kappa receptor. Dynorphin (1-8) inhibits the binding of ³H-Bremazocine to purified kappa receptors with an IC50 of 303 nM. Activation of KOR by dynorphin peptides mediates various physiological effects, including pain modulation, stress responses, and reward processing.
|
|---|---|
| ln Vitro |
In vitro, dynorphin (1-8) is an opioid peptide that binds to the kappa opioid receptor with high affinity. It inhibits the binding of ³H-Bremazocine to purified kappa receptors with an IC50 of 303 nM. It is the major opioid peptide in placental tissue extracts. In cell-based assays, dynorphin (1-8) activates KOR-mediated signaling pathways, such as the inhibition of adenylyl cyclase and the activation of MAPK pathways. Its activity can be blocked by selective KOR antagonists such as nor-binaltorphimine (nor-BNI).
|
| ln Vivo |
In vivo, dynorphin (1-8) is an endogenous neuropeptide that plays a role in pain modulation, stress responses, and addiction. It is derived from the precursor protein prodynorphin, which is expressed in the central nervous system and peripheral tissues. As a KOR agonist, it produces analgesia (pain relief) at the spinal level but can also produce dysphoria and aversive effects at supraspinal sites. It has been shown to have a wide range of biological activities, including modulation of neurotransmitter release and immune function.
|
| Enzyme Assay |
Non-cellular in vitro assays for dynorphin (1-8) involve receptor binding studies. A standard protocol uses membrane preparations from cells expressing recombinant human kappa opioid receptors. The membranes are incubated with a radiolabeled ligand, such as [³H]bremazocine or [³H]U-69593, and varying concentrations of dynorphin (1-8). Non-specific binding is determined in the presence of an excess of unlabeled ligand (e.g., nor-BNI). After incubation, the reaction is terminated by rapid filtration, and the radioactivity bound to the membranes is measured. The IC50 or Ki values are calculated from the competition curves.
|
| Cell Assay |
Cellular assays for dynorphin (1-8) are performed using cell lines expressing kappa opioid receptors, such as CHO cells or HEK293 cells stably transfected with KOR. Cells are pre-incubated with dynorphin (1-8) at various concentrations. The inhibition of forskolin-stimulated cAMP accumulation is measured using a competitive ELISA or a homogeneous time-resolved fluorescence (HTRF) assay. The EC50 for receptor activation is determined from the concentration-response curve. The involvement of KOR can be confirmed using selective antagonists.
|
| Animal Protocol |
In vivo animal studies for dynorphin (1-8) are conducted in rodent models of pain, such as the tail-flick test or the hot plate test. Animals are administered dynorphin (1-8) via intrathecal or intracerebroventricular injection at doses such as 1-10 nmol. The latency to respond to a thermal stimulus is measured. The analgesic effect is assessed. The compound's effects on reward and aversion can be studied using conditioned place preference (CPP) or conditioned place aversion (CPA) paradigms.
|
| ADME/Pharmacokinetics |
Dynorphin (1-8) is a peptide with a molecular weight of 981.15 and a molecular formula of C46H72N14O10. As a peptide, it has poor oral bioavailability and is typically administered via injection (intrathecal, intracerebroventricular, or intravenous) in animal studies. It is degraded by peptidases in the circulation and tissues, leading to a short half-life. It is stored as a powder at -20°C. Its solubility in water is limited but can be enhanced with mild acid or DMSO.
|
| Toxicity/Toxicokinetics |
Detailed toxicological data for dynorphin (1-8) have not been extensively reported. As a research peptide, it is not intended for human use and is strictly for preclinical research purposes. Standard safety precautions should be followed when handling dynorphin (1-8), including the use of personal protective equipment. No specific toxicity data, such as LD50 values, are available in the provided literature.
|
| References | |
| Additional Infomation |
Dynorphin (1-8) is an endogenous opioid peptide that is the major opioid peptide in placental tissue extracts and is the most likely natural ligand for the kappa opioid receptor. It comprises the N-terminal eight residues of dynorphin A. It has been shown to have a wide range of biological activities, including pain modulation, stress responses, and regulation of neurotransmitter release. The peptide is used as a research tool to study kappa opioid receptor signaling and its role in various physiological and pathophysiological processes. It is not a clinically approved drug and has not entered clinical trials.
|
| Molecular Formula |
C46H72N14O10
|
|---|---|
| Molecular Weight |
981.17
|
| Exact Mass |
980.556
|
| CAS # |
75790-53-3
|
| PubChem CID |
10486131
|
| Appearance |
White to off-white solid powder
|
| Density |
1.38g/cm3
|
| Index of Refraction |
1.637
|
| LogP |
3.682
|
| Hydrogen Bond Donor Count |
14
|
| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
31
|
| Heavy Atom Count |
70
|
| Complexity |
1760
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
CC[C@@H]([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC(CNC([C@@H](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(O)=O)C
|
| InChi Key |
WRPLGMBDXVBPEG-VGXZEHLRSA-N
|
| InChi Code |
InChI=1S/C46H72N14O10/c1-5-27(4)38(44(69)70)60-41(66)33(14-10-20-53-46(50)51)57-40(65)32(13-9-19-52-45(48)49)58-42(67)34(21-26(2)3)59-43(68)35(23-28-11-7-6-8-12-28)56-37(63)25-54-36(62)24-55-39(64)31(47)22-29-15-17-30(61)18-16-29/h6-8,11-12,15-18,26-27,31-35,38,61H,5,9-10,13-14,19-25,47H2,1-4H3,(H,54,62)(H,55,64)(H,56,63)(H,57,65)(H,58,67)(H,59,68)(H,60,66)(H,69,70)(H4,48,49,52)(H4,50,51,53)/t27-,31-,32-,33-,34-,35-,38-/m0/s1
|
| Chemical Name |
(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-methylpentanoic acid
|
| Synonyms |
PH-8PDynorphin (1-8)
|
| HS Tariff Code |
2934.99.9001
|
| 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 (e.g. under nitrogen), 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)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~101.92 mM)
|
|---|---|
| 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 | 1.0192 mL | 5.0960 mL | 10.1919 mL | |
| 5 mM | 0.2038 mL | 1.0192 mL | 2.0384 mL | |
| 10 mM | 0.1019 mL | 0.5096 mL | 1.0192 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04108546 | RECRUITING | Device: Electroacupuncture device Drug: Epidural analgesia |
Anesthesia, Local Back Pain Electroacupuncture Epidural |
University of Thessaly | 2020-02-01 | Not Applicable |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
