| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Kappa-opioid receptor (KOR / OPRK1). Rimorphin exhibits the highest binding affinity for KOR among the dynorphin peptides. It also binds to mu-opioid receptors (MOR) and delta-opioid receptors (DOR) with lower affinity. As a KOR agonist, Rimorphin activates G-protein-coupled signaling pathways that modulate pain perception, mood, and neuroendocrine function.
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| ln Vitro |
Dynorphin B (1-13) is a highly effective 13-amino acid opioid peptide. Research on the neurophysiological effects of dynorphin B (1–13) has been conducted in large quantities [1].
In vitro, Rimorphin demonstrates potent agonist activity at the kappa-opioid receptor. It is widely utilized in receptor binding studies to characterize the pharmacological properties of KOR. The peptide activates nuclear opioid receptors coupling nuclear protein kinase C activation to the transcription of cardiogenic genes in embryonic stem cells. Its affinity and potency at KOR make it a valuable tool for studying opioid receptor pharmacology. |
| ln Vivo |
In vivo, Rimorphin produces potent analgesic effects through activation of kappa-opioid receptors in the central nervous system. Its neurophysiological actions have been extensively studied, revealing roles in pain modulation, stress-induced analgesia, and regulation of mood and behavior. The peptide's effects are mediated through both central and peripheral KOR activation, with distinct pharmacological profiles compared to mu-opioid receptor agonists.
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| Enzyme Assay |
Cell-free receptor binding assays for Rimorphin typically use membrane preparations from cells expressing recombinant human kappa-opioid receptors or from brain tissue rich in KOR. The peptide is incubated with a radiolabeled KOR-selective ligand (e.g., [³H]-U69,593) at varying concentrations for 60-120 minutes at room temperature. Nonspecific binding is determined in the presence of an excess of unlabeled KOR agonist. Bound and free radioactivity are separated by filtration through glass fiber filters, and Ki values are calculated from competition curves using nonlinear regression analysis.
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| Cell Assay |
Cellular functional assays for Rimorphin utilize cell lines stably expressing the kappa-opioid receptor (e.g., CHO-KOR or HEK-293-KOR cells). Cells are seeded in 96-well plates and treated with Rimorphin at concentrations ranging from 0.01 nM to 10 μM. Receptor activation is measured by monitoring the inhibition of forskolin-stimulated cAMP accumulation via HTRF or ELISA-based cAMP assays. Alternatively, G-protein activation is assessed using [³⁵S]GTPγS binding assays. EC50 values are determined from dose-response curves. Antagonist studies can be performed by pre-incubating cells with selective KOR antagonists prior to agonist addition.
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| Animal Protocol |
In vivo animal studies with Rimorphin are typically performed in rodents via intracerebroventricular (ICV), intrathecal (IT), or systemic administration. The peptide is administered at doses ranging from 0.1-10 nmol for ICV or IT routes. Analgesic effects are assessed using standard pain models such as the tail-flick test, hot plate test, or formalin test. Behavioral assays including the forced swim test or elevated plus maze are used to evaluate mood and anxiety-related effects. Receptor selectivity is confirmed by pre-treatment with selective KOR antagonists (e.g., nor-binaltorphimine) to block Rimorphin-induced effects. Tissue distribution and peptide stability are assessed by measuring peptide levels in brain and plasma via ELISA or LC-MS/MS.
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| ADME/Pharmacokinetics |
As a peptide, Rimorphin has limited oral bioavailability and is typically administered via parenteral routes (ICV, IT, or intravenous) in research settings. Its plasma half-life is longer than that of native bradykinin but still relatively short due to rapid enzymatic degradation by peptidases. The peptide is metabolized by various proteases in the blood and tissues. Its distribution is primarily to the central nervous system when administered centrally, with limited peripheral penetration due to the blood-brain barrier.
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| Toxicity/Toxicokinetics |
Toxicological data for Rimorphin are limited to research studies. As an endogenous opioid peptide, it is generally well-tolerated at physiological concentrations. At pharmacological doses, KOR activation can produce dysphoria, sedation, and diuretic effects. Standard safety pharmacology studies would be required for clinical development. The peptide is handled with standard laboratory precautions for bioactive compounds. No significant organ toxicity has been reported in published literature at research-grade doses.
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| References | |
| Additional Infomation |
Dynorphin B is the main leucine enkephalin in tissues containing dynorphin and α-neoendorphin.
Rimorphin / Dynorphin B (1-13) is a well-characterized research tool for studying kappa-opioid receptor pharmacology. It is not an approved therapeutic agent and has not entered clinical trials as a drug candidate. The peptide is available from biochemical suppliers for research purposes only. Its high potency and selectivity for KOR make it a valuable probe for investigating the physiological and pathological roles of the kappa-opioid system. The peptide is typically stored lyophilized at -20°C and reconstituted in appropriate buffers for experimental use. |
| Molecular Formula |
C74H115N21O17
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|---|---|
| Molecular Weight |
1570.86
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| Exact Mass |
1569.88
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| CAS # |
83335-41-5
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| Related CAS # |
Dynorphin B (1-13) (TFA)
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| PubChem CID |
25075991
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| Appearance |
White to off-white solid powder
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| LogP |
4.745
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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 |
51
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| Heavy Atom Count |
112
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| Complexity |
3110
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@H]([C@@H](C(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)CNC(=O)CNC(=O)[C@H](CC3=CC=C(C=C3)O)N)O
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| InChi Key |
AGTSSZRZBSNTGQ-ITZCFHCWSA-N
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| InChi Code |
InChI=1S/C74H115N21O17/c1-40(2)34-53(91-68(107)54(36-44-18-10-8-11-19-44)86-58(100)39-84-57(99)38-85-62(101)48(76)35-46-25-27-47(97)28-26-46)67(106)89-51(24-17-33-83-74(80)81)63(102)87-50(23-16-32-82-73(78)79)64(103)90-52(29-30-56(77)98)65(104)92-55(37-45-20-12-9-13-21-45)69(108)88-49(22-14-15-31-75)66(105)93-59(41(3)4)70(109)94-60(42(5)6)71(110)95-61(43(7)96)72(111)112/h8-13,18-21,25-28,40-43,48-55,59-61,96-97H,14-17,22-24,29-39,75-76H2,1-7H3,(H2,77,98)(H,84,99)(H,85,101)(H,86,100)(H,87,102)(H,88,108)(H,89,106)(H,90,103)(H,91,107)(H,92,104)(H,93,105)(H,94,109)(H,95,110)(H,111,112)(H4,78,79,82)(H4,80,81,83)/t43-,48+,49+,50+,51+,52+,53+,54+,55+,59+,60+,61+/m1/s1
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| Chemical Name |
(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-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]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoic acid
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| Synonyms |
Dynorphin B; Rimorphin
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~31.83 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 | 0.6366 mL | 3.1830 mL | 6.3659 mL | |
| 5 mM | 0.1273 mL | 0.6366 mL | 1.2732 mL | |
| 10 mM | 0.0637 mL | 0.3183 mL | 0.6366 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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