| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
EphA4 4.22 μM μM (IC50) EphA4 1.30 μM (Ki)
KYL peptide targets the EphA4 receptor tyrosine kinase. It binds to the ligand-binding domain of EphA4, antagonizing its interaction with its ligand, EphrinA5. By blocking EphA4 activation, the peptide prevents downstream signaling that can lead to dendritic spine loss, synaptic damage, and impairment of long-term potentiation (LTP), which are key processes in neurodegeneration and cognitive decline. |
|---|---|
| ln Vitro |
The KYL peptide eliminates the Aβ-stimulated EphA4 tyrosine phosphorylation by blocking the extracellular ligand-binding domain of EphA4[2]. In cultured hippocampal neurons, the Aβ-triggered reduction of dendritic spines is eliminated by KYL peptide[2].
In vitro, KYL peptide has been shown to prevent AβO (amyloid-beta oligomer)-induced dendritic spine loss and synaptic damage. It also prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. These activities are typically assessed using neuronal cell cultures and electrophysiological recordings. The peptide's neuroprotective effects are attributed to its ability to inhibit EphA4 signaling. |
| ln Vivo |
In vivo, KYL peptide has demonstrated neuroprotective effects in animal models of neurological disorders. While specific in vivo data is limited, its ability to prevent synaptic damage and LTP impairment suggests potential therapeutic benefits in conditions like Alzheimer's disease. The peptide shows a long half-life in cell culture media, which may translate to favorable pharmacokinetics in vivo.
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| Enzyme Assay |
Cell-free assays for KYL peptide typically involve measuring its binding affinity to EphA4 using surface plasmon resonance (SPR) or radioligand binding assays. The Kd value of 0.8 μM is determined using these techniques. Additionally, competitive binding assays are used to measure the IC50 for inhibition of EphA4-EphrinA5 interactions.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of KYL peptide. Neuronal cultures are treated with the peptide in the presence of AβO. Dendritic spine density and synaptic protein levels are measured to assess protection against AβO-induced damage. Electrophysiological recordings are used to measure LTP in hippocampal slices to evaluate the peptide's ability to prevent LTP impairment.
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| Animal Protocol |
In vivo animal experiments typically involve rodent models of Alzheimer's disease or other neurodegenerative conditions. Animals are administered KYL peptide. Cognitive function is assessed using behavioral tests, and markers of synaptic damage and neurodegeneration are measured in brain tissues. These studies provide evidence for the peptide's neuroprotective effects.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of KYL peptide are characteristic of a peptide. Its molecular weight is 1465.75. It is soluble in water (2 mg/mL). It shows a long half-life in cell culture media, suggesting good stability. While detailed in vivo PK parameters are not widely published, its stability supports its use in research applications.
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| Toxicity/Toxicokinetics |
The toxicity profile of KYL peptide is not extensively documented. As a peptide, it is generally considered to have low toxicity. In preclinical studies, the peptide has been shown to be well-tolerated at the doses tested, with a safety profile that supports its use in research.
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| References |
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| Additional Infomation |
KYL peptide is a selective EphA4 receptor antagonist with neuroprotective properties. It prevents AβO-induced dendritic spine loss and synaptic damage, and it prevents the blocking of LTP. The peptide is used in research to study the role of EphA4 in neurodegenerative diseases and to develop potential therapeutic strategies. It is not approved for therapeutic use.
|
| Molecular Formula |
C74H108N14O17
|
|---|---|
| Molecular Weight |
1465.73293876648
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| Exact Mass |
1464.801
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| CAS # |
676657-00-4
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| PubChem CID |
91691122
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| Appearance |
White to off-white solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
17
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
40
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| Heavy Atom Count |
105
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| Complexity |
2890
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| Defined Atom Stereocenter Count |
12
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| SMILES |
O=C([C@H](CC(C)C)NC([C@H](CC1C=CC(=CC=1)O)NC([C@H](CCCCN)N)=O)=O)N1CCC[C@H]1C(N[C@@H](CC1C=CC(=CC=1)O)C(N[C@@H](CC1=CNC2C=CC=CC1=2)C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(=O)O)CC(C)C)=O)CO)=O)CO)=O)CC(C)C)=O)C(C)C)=O)=O)=O)=O
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| InChi Key |
FZNPYIAZMDBRLC-RKNDTPCJSA-N
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| InChi Code |
InChI=1S/C74H108N14O17/c1-40(2)31-52(64(94)84-59(39-90)68(98)85-58(38-89)67(97)83-57(74(104)105)33-42(5)6)80-71(101)62(43(7)8)86-70(100)61-19-14-30-88(61)73(103)56(36-46-37-77-51-17-10-9-15-49(46)51)82-66(96)54(35-45-22-26-48(92)27-23-45)79-69(99)60-18-13-29-87(60)72(102)55(32-41(3)4)81-65(95)53(34-44-20-24-47(91)25-21-44)78-63(93)50(76)16-11-12-28-75/h9-10,15,17,20-27,37,40-43,50,52-62,77,89-92H,11-14,16,18-19,28-36,38-39,75-76H2,1-8H3,(H,78,93)(H,79,99)(H,80,101)(H,81,95)(H,82,96)(H,83,97)(H,84,94)(H,85,98)(H,86,100)(H,104,105)/t50-,52-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoic acid
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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: ≥ 55 mg/mL (37.52 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 | 0.6823 mL | 3.4113 mL | 6.8225 mL | |
| 5 mM | 0.1365 mL | 0.6823 mL | 1.3645 mL | |
| 10 mM | 0.0682 mL | 0.3411 mL | 0.6823 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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