| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Kyotorphin's mechanism of action is complex and not fully understood. It is known to exert analgesic effects by releasing endogenous enkephalins (Met-enkephalin and Leu-enkephalin), which are endogenous opioid peptides. This indirect activation of the opioid system contributes to its pain-relieving properties. Kyotorphin also has direct effects on the central nervous system, including anti-inflammatory and neuroprotective actions. It is synthesized at nerve terminals and is found in the brain and CSF. Its levels are altered in certain pathological conditions.
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| ln Vitro |
Using the hot plate test, the analgesic efficacy of Kyotomorphin was determined. Its ED50 value was found to be 5.3 μg/animal (15.7 nmole/animal) [1].
In vitro, Kyotorphin has been shown to have anti-inflammatory and antibacterial activities. Its effects on pain pathways can be studied in neuronal cultures. However, specific in vitro data, such as IC50 or EC50 values, are not detailed in standard product descriptions. The compound is used as a research tool to study its effects on neuronal signaling and inflammation. |
| ln Vivo |
In vivo, Kyotorphin has been shown to have analgesic effects in animal models of pain. It is believed to exert its effects by releasing endogenous enkephalins. Its levels in the CSF are altered in conditions such as persistent pain and Alzheimer's disease. However, specific in vivo protocols and results, such as efficacy in pain models, are not detailed in standard product descriptions. Its use is limited to research applications.
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| Enzyme Assay |
The in vitro assays for Kyotorphin measure its binding to its targets and its effects on enkephalin release. Receptor binding assays can be performed to study its interaction with potential receptors. Functional assays can measure the release of enkephalins from neuronal preparations. However, specific protocols are not detailed in standard product descriptions. The compound is a research tool.
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| Cell Assay |
In vitro cell-based assays for Kyotorphin are used to study its effects on neuronal cells. In a typical assay, neuronal cultures are treated with Kyotorphin, and the release of enkephalins is measured by ELISA. The compound's effects on cell viability and inflammation can also be assessed. These assays confirm its activity in a cellular context.
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| Animal Protocol |
In vivo animal experiments for Kyotorphin are conducted in models of pain. In a typical study, Kyotorphin is administered to animals, and its analgesic effects are assessed using tests such as the tail-flick or hot-plate test. The compound's ability to reduce pain responses is measured. These studies confirm its analgesic activity.
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| ADME/Pharmacokinetics |
Kyotorphin has a molecular weight of 337.37 g/mol and a molecular formula of C15H23N5O4. It is a solid compound. It is soluble in water and other solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a peptide, it is likely to be rapidly degraded in vivo.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Kyotorphin is not provided in standard product descriptions. As an endogenous peptide, it is generally considered to have low toxicity. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling Kyotorphin. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
Tyr-Arg is a dipeptide composed of L-tyrosine and L-arginine linked by a peptide bond. It is the conjugate base of L-tyrosinyl-L-arginine (1+).
Kyotorphin is a research compound and is not approved for any clinical or therapeutic use. It is an endogenous neuroactive dipeptide with analgesic, anti-inflammatory, and antibacterial activities. It is composed of L-tyrosine and L-arginine. Kyotorphin is synthesized at nerve terminals and is found in the brain and cerebrospinal fluid (CSF). People with persistent pain and Alzheimer's disease have lower levels of kyotorphin in their CSF. Its mechanism of action involves releasing endogenous enkephalins. Kyotorphin is a valuable research tool for studying pain, neuroprotection, and neuroinflammation. |
| Molecular Formula |
C15H23N5O4
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|---|---|
| Molecular Weight |
337.38
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| Exact Mass |
337.175
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| CAS # |
70904-56-2
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| PubChem CID |
123804
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| Appearance |
White to off-white solid powder
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| Density |
1.43 g/cm3
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| LogP |
1.376
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
24
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| Complexity |
445
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1=CC(=CC=C1C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)N)O
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| InChi Key |
JXNRXNCCROJZFB-RYUDHWBXSA-N
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| InChi Code |
InChI=1S/C15H23N5O4/c16-11(8-9-3-5-10(21)6-4-9)13(22)20-12(14(23)24)2-1-7-19-15(17)18/h3-6,11-12,21H,1-2,7-8,16H2,(H,20,22)(H,23,24)(H4,17,18,19)/t11-,12-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid
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| Synonyms |
L-Tyrosyl-L-arginineKyotorphin KiotorphinTyr-arg
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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 : ~125 mg/mL (~370.51 mM)
H2O : ~100 mg/mL (~296.41 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.17 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 20.8 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: ≥ 2.08 mg/mL (6.17 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 20.8 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: ≥ 2.08 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (74.10 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9640 mL | 14.8201 mL | 29.6402 mL | |
| 5 mM | 0.5928 mL | 2.9640 mL | 5.9280 mL | |
| 10 mM | 0.2964 mL | 1.4820 mL | 2.9640 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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