| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
The target of NEP(1-40) is the Nogo-66 receptor (NgR), a GPI-anchored protein expressed on the surface of neurons in the central nervous system (CNS). NgR is a receptor for three myelin-associated inhibitors: Nogo-A, MAG (myelin-associated glycoprotein), and OMgp (oligodendrocyte myelin glycoprotein). Binding of these inhibitors to NgR activates a signaling cascade involving RhoA, leading to growth cone collapse and inhibition of axonal outgrowth. NEP(1-40) acts as a competitive antagonist by binding to NgR and blocking the interaction with the inhibitory ligands. It thereby promotes axonal regeneration after CNS injury.
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| ln Vitro |
In vitro, NEP(1-40) (0.1-10 uM) blocks Nogo-66 or CNS myelin inhibition of axonal outgrowth in neuronal cultures. It reverses the injury-induced shift in the distribution of microglia morphologies by limiting myelin-based inhibition. The peptide has neuroprotective effects and promotes neurite outgrowth in cerebellar granule neurons and dorsal root ganglion (DRG) neurons cultured on myelin substrates. It does not have direct cytotoxic effects on neurons.
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| ln Vivo |
In vivo, NEP(1-40) promotes axonal regeneration and functional recovery in animal models of spinal cord injury (SCI) and stroke. In rats with spinal cord contusion injury, intrathecal administration of NEP1-40 promotes axonal sprouting, reduces cavitation, and improves locomotor recovery. It also reverses the injury-induced shift in microglia morphology, limiting myelin-based inhibition. The peptide is a research tool for studying NgR-mediated inhibition and has potential therapeutic applications for CNS injury and stroke, but it is not an approved drug.
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| Enzyme Assay |
The binding of NEP(1-40) to NgR can be assessed by surface plasmon resonance (SPR). Recombinant human NgR-Fc fusion protein is immobilized on a CM5 sensor chip. Varying concentrations of NEP(1-40) (0.01-100 uM) are injected over the chip in running buffer (PBS, pH 7.4, 0.05% Tween-20). The association (kon) and dissociation (koff) rates are recorded, and the Kd is calculated. For competition assays, labeled Nogo-66 peptide is used as a competitor.
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| Cell Assay |
For neurite outgrowth assays, cerebellar granule neurons or dorsal root ganglion (DRG) neurons are isolated from postnatal rats. Myelin substrates are prepared by coating coverslips with CNS myelin (10-50 ug/mL). Neurons are seeded in 24-well plates and cultured in the presence of NEP(1-40) (0.1-10 uM) for 24-48 h. Neurons are fixed and stained with anti-neurofilament antibody or betaIII-tubulin antibody. Neurite length is measured using ImageJ software. For microglia morphology studies, microglial cells are isolated from neonatal rat brains and cultured on myelin substrates with NEP(1-40) (1-10 uM), and cell morphology (round vs. amoeboid vs. ramified) is assessed by Iba-1 immunohistochemistry.
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| Animal Protocol |
Spinal cord injury (SCI) rat model: Female Sprague-Dawley rats (200-250 g, n=10-12/group) are subjected to moderate spinal cord contusion injury at T9-T10 using a NYU impactor. NEP(1-40) (10-100 ug) is administered intrathecally via a catheter implanted at the level of the injury, beginning immediately or 1 h post-injury, once daily for 7-14 days. Control groups receive vehicle (PBS) or a scrambled control peptide. Locomotor function is assessed using the Basso, Beattie, Bresnahan (BBB) locomotor rating scale at 1, 3, 7, 14, 21, 28 days post-injury. At the endpoint, spinal cords are harvested for histology (H&E, Luxol fast blue for myelin), immunohistochemistry (neurofilament for axons, GFAP for astrocytes, Iba-1 for microglia, GAP-43 for axonal sprouting), and lesion volume measurement. For stroke models, NEP(1-40) is administered intracerebroventricularly (ICV).
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| ADME/Pharmacokinetics |
No specific PK data for NEP(1-40) is available. As a 40-amino acid peptide (MW 4625.11), it has a very short plasma half-life (< 30 min) due to proteolytic degradation and renal clearance. For in vivo studies, it is administered intrathecally to bypass the blood-brain barrier and to achieve local concentrations in the CNS. For research use, it is stored as a lyophilized powder at -20degC (powder: -80degC for 2 years, -20degC for 1 year; in solvent: -80degC for 6 months, -20degC for 1 month). It is soluble in DMSO and water (as TFA salt).
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| Toxicity/Toxicokinetics |
No specific toxicology data for NEP(1-40) is available. In animal studies at effective doses (10-100 ug, intrathecal), no overt toxicity has been reported. Standard safety precautions for handling peptides apply: use PPE (gloves, lab coat, safety goggles), work in a fume hood, avoid inhalation and skin contact. Not for human consumption.
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| References | |
| Additional Infomation |
NEP(1-40), N-terminal uncapped (Nogo-66 receptor antagonist peptide; CAS# 475221-20-6; MW 4625.11; sequence RIYKGVIQAIQKSDEGHPFRAYLESEVAISEELVQKYSNS-NH2) is a research-grade NgR antagonist peptide used for promoting axonal regeneration after CNS injury. It is not an FDA-approved drug. It is used in studies of spinal cord injury, stroke, neuroregeneration, and myelin-based inhibition. For research use only, not for diagnostic or therapeutic applications. Storage: powder at -80degC for 2 years, -20degC for 1 year; in solvent at -80degC for 6 months, -20degC for 1 month.
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| Molecular Formula |
C204H322N56O64
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| Molecular Weight |
4583.08
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| Appearance |
White to off-white solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.2182 mL | 1.0910 mL | 2.1819 mL | |
| 5 mM | 0.0436 mL | 0.2182 mL | 0.4364 mL | |
| 10 mM | 0.0218 mL | 0.1091 mL | 0.2182 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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