| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
| Targets |
The targets of Pinealon primarily involve oxidative stress and signal transduction pathways. This peptide prevents reactive oxygen species accumulation and suppresses ERK 1/2 activation. By inhibiting the ERK signaling pathway, Pinealon reduces spontaneous cell death and protects neurons from damage. Studies indicate that Pinealon restricts lipid peroxidation by modifying lipoprotein structure and increases red blood cell membrane stability against osmotic hemolysis
Pinealon targets ROS (Reactive Oxygen Species) and the ERK 1/2 signaling pathway. By preventing ROS accumulation and inhibiting ERK 1/2 activation, it protects neurons from oxidative stress and apoptosis. Its neuroprotective effects are mediated through the modulation of these key cellular pathways, which are involved in neuronal survival and function. |
|---|---|
| ln Vitro |
In a dose-dependent manner, pinealon (10, 50, and 100 nM; 30 min) inhibits the increase in ROS accumulation in cerebellar granule cells caused by ouabain [1]. Rat cerebellar granule cells exposed to 500 mM homocysteine (HC) are shown to exhibit inhibited ERK 1/2 activation in response to pinealon (10 nM; 0, 2.5, 5, 10, 20, 30 min) [1].
In vitro studies demonstrate that Pinealon exhibits significant cytoprotective activity in various models. In ouabain-injured cerebellar granule cells, Pinealon (10, 50, 100 nM for 30 minutes) inhibits the increase in ROS accumulation in a dose-dependent manner. In rat cerebellar granule cells treated with homocysteine (500 mM), Pinealon (10 nM) inhibits ERK 1/2 activation. Furthermore, Pinealon stimulates the functional activity of major cellular components of brain tissue and reduces spontaneous cell death levels. Studies indicate that short peptides restrict lipid peroxidation by modifying lipoprotein structure and increase neuronal population survival. In vitro, Pinealon has been shown to prevent ROS buildup and inhibit ERK 1/2 activation. Its neuroprotective properties are typically assessed using neuronal cell cultures subjected to oxidative stress. These studies confirm its ability to protect neurons from damage and promote cell survival. |
| ln Vivo |
Pinealon (50, 100, 200 ng/kg; Injection, for 5 days) shows a dose-dependent effect on the maintenance of previously acquired skills in rats[2]. Pinealon (10 µg/kg; daily for 5 days) protects rat offspring from prenatal hyperhomocysteinemia[3].
In vivo studies demonstrate that Pinealon exhibits protective effects on cognition and development. In rats, Pinealon (50, 100, 200 ng/kg, injection for 5 days) shows a dose-dependent effect on the maintenance of a previously acquired skill. More importantly, Pinealon (10 µg/kg, daily for 5 days) protects rat offspring from prenatal hyperhomocysteinemia, demonstrating neuroprotective effects. Studies also indicate that Pinealan reduces spontaneous cell death levels and stimulates the functional activity of major cellular components of brain tissue. In vivo, Pinealon (50, 100, 200 ng/kg; Injection, for 5 days) shows a dose-dependent effect on the maintenance of a previously acquired skill in rats. This demonstrates its ability to support cognitive function and neuroprotection in vivo. Its effects are attributed to its ability to reduce oxidative stress and modulate signaling pathways in the brain. |
| Enzyme Assay |
Cell-free assays for Pinealon primarily focus on direct protein interactions. A typical protocol includes: 1) Prepare a reaction system containing target proteins (such as ERK kinase or lipoproteins); 2) Dissolve Pinealon in appropriate buffer (e.g., PBS pH 7.4) to prepare various concentrations (0-100 μM); 3) Incubate at 37°C for a certain period (typically 15-60 minutes); 4) Detect binding affinity using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC); 5) To assess effects on lipid peroxidation, incubate Pinealon with human plasma low-density lipoprotein (LDL) and detect lipid peroxidation products using the fluorescent probe C11-BODIPY.
Cell-free assays for Pinealon typically involve measuring its antioxidant activity using chemical assays such as DPPH or ABTS radical scavenging assays. Its ability to inhibit ERK 1/2 activation can be assessed using kinase activity assays. These assays are used to characterize the compound's mechanism of action. |
| Cell Assay |
The in vitro cell assay protocol for Pinealon is as follows: 1) Seed target cells (such as primary cerebellar granule cells, neuronal cell lines, or red blood cells) in culture plates and culture to appropriate density at 37°C with 5% CO₂; 2) Pre-treat cells with various concentrations of Pinealon (typically 1-100 nM) for 30 minutes; 3) Expose to injury conditions: ouabain (to induce oxidative stress) or homocysteine (500 mM) treatment; 4) Measure intracellular ROS levels using specific fluorescent probes (e.g., DCFH-DA); 5) Detect ERK 1/2 phosphorylation levels by Western blot; 6) Assess cell death rate using trypan blue staining or Annexin V/PI double staining; 7) Evaluate red blood cell membrane stability by measuring osmotic fragility.
In vitro cellular assays are conducted to evaluate the functional activity of Pinealon. Neuronal cells are treated with the peptide in the presence of oxidative stress, and cell viability is measured to assess its neuroprotective effects. ROS levels are measured to confirm its antioxidant activity. ERK 1/2 phosphorylation is measured to assess the inhibition of this signaling pathway. |
| Animal Protocol |
Animal/Disease Models: 200-250 g, white male rats[2]
Doses: 50, 100, 200 ng/kg Route of Administration: Injection; for 5 days Experimental Results: demonstrated dose-dependent effects on the maintenance of a previously acquired skill in the Morris maze. Animal/Disease Models: 180-200 g, Female Wistar rats[3] Doses: 10 µg/kg Route of Administration: Ip; daily for 5 days Experimental Results: Protected the rat offspring from prenatal hyperhomocysteinemia. The in vivo animal assay protocol for Pinealon is as follows: 1) Use rats (adult or pregnant) as experimental animals; 2) Establish cognitive or developmental impairment models (such as prenatal hyperhomocysteinemia model); 3) Randomize animals into vehicle control and multiple Pinealon treatment groups (e.g., 50, 100, 200 ng/kg or 10 µg/kg); 4) Administration routes: intraperitoneal or intravenous injection, once daily for 5 days; 5) Behavioral testing: assess cognitive function and skill maintenance using tests such as conditioned active avoidance response; 6) Euthanize animals at study termination and collect brain tissue for histopathological examination; 7) Measure oxidative stress markers and neuronal survival in brain tissue. In vivo animal experiments typically involve rodent models of neurodegenerative diseases or cognitive impairment. Animals are administered Pinealon via injection. Cognitive function is assessed using behavioral tests, and markers of oxidative stress and neuronal survival are measured in brain tissues. These studies provide evidence for the compound's neuroprotective effects. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies of Pinealon are limited. As a small-molecule tripeptide (molecular weight 418.4 Da), Pinealon has favorable tissue penetration properties. In in vivo studies, effective doses range from 50-200 ng/kg, indicating high biological activity of this peptide. Due to its low molecular weight and peptide structure, Pinealon likely distributes rapidly to brain tissue. The compound is typically administered via injection (intraperitoneal or intravenous), once daily for several days. Stability studies indicate that short peptides exert their biological effects by modifying lipoprotein structure, suggesting possible interaction with plasma proteins. Systematic data on half-life, metabolic pathways, and excretion are not detailed in the current literature.
The pharmacokinetic properties of Pinealon are characteristic of a small peptide. Its molecular weight is 418.40. As a tripeptide, it is likely to be rapidly metabolized and cleared from the circulation. Its ability to exert effects in the brain suggests it may cross the blood-brain barrier, although its precise pharmacokinetic profile is not well-characterized. |
| Toxicity/Toxicokinetics |
According to the Material Safety Data Sheet, Pinealon is classified as a non-hazardous substance or mixture with no GHS hazard classification identified. The compound is not classified as a carcinogen by NTP, IARC, OSHA, or ACGIH. Pinealon is for research use only and is not intended for human or veterinary use. The peptide has not received FDA approval for any medical use. No significant toxicity has been reported in animal studies within the effective dose range. However, the dual regulatory effect of this peptide on apoptotic processes should be approached with caution; its pro-apoptotic activity may have cancer-promoting potential when the apoptotic process does not function correctly. Pregnant or breastfeeding mothers should avoid using this compound, as sufficient safety evidence is not available.
The toxicity profile of Pinealon is not extensively documented. As a naturally occurring peptide, it is generally considered to have low toxicity. In preclinical studies, the compound has been shown to be well-tolerated at the doses tested, with a safety profile that supports its use in research. |
| References |
|
| Additional Infomation |
Glu-Asp-Arg is a tripeptide composed of L-glutamic acid, L-aspartic acid, and L-arginine linked by peptide bonds. It possesses neuroprotective properties, similar to those of L-aspartic acid, L-glutamic acid, and L-arginine.
Pinealon is a tripeptide (Glu-Asp-Arg) with neuroprotective properties. It prevents ROS buildup and inhibits ERK 1/2 activation. It is being studied for its potential to support cognitive function and protect against neurodegenerative diseases. It is a research compound and is not approved for therapeutic use. |
| Molecular Formula |
C15H26N6O8
|
|---|---|
| Molecular Weight |
418.40
|
| Exact Mass |
418.181
|
| Elemental Analysis |
C, 43.06; H, 6.26; N, 20.09; O, 30.59
|
| CAS # |
175175-23-2
|
| PubChem CID |
10273502
|
| Sequence |
H-Glu-Asp-Arg-OH; L-alpha-glutamyl-L-alpha-aspartyl-L-arginine
|
| SequenceShortening |
EDR
|
| Appearance |
White to off-white solid powder
|
| LogP |
-6.1
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
29
|
| Complexity |
649
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C(C[C@@H](C(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)N)CN=C(N)N
|
| InChi Key |
QPRZKNOOOBWXSU-CIUDSAMLSA-N
|
| InChi Code |
InChI=1S/C15H26N6O8/c16-7(3-4-10(22)23)12(26)21-9(6-11(24)25)13(27)20-8(14(28)29)2-1-5-19-15(17)18/h7-9H,1-6,16H2,(H,20,27)(H,21,26)(H,22,23)(H,24,25)(H,28,29)(H4,17,18,19)/t7-,8-,9-/m0/s1
|
| Chemical Name |
(4S)-4-amino-5-[[(2S)-3-carboxy-1-[[(1S)-1-carboxy-4-(diaminomethylideneamino)butyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
|
| Synonyms |
lu-Asp-Arg; glutamyl-aspartyl-arginine; CHEBI:156374; L-Glutamyl-L-aspartyl-L-arginine;
|
| 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 |
| 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 (239 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 | 2.3901 mL | 11.9503 mL | 23.9006 mL | |
| 5 mM | 0.4780 mL | 2.3901 mL | 4.7801 mL | |
| 10 mM | 0.2390 mL | 1.1950 mL | 2.3901 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA