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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Tet1-Cys peptide targets the trisialoganglioside GT1b (a complex glycosphingolipid) expressed on the surface of neurons. The specificity is for neurons; it does not bind to glial cells or non-neuronal cells. The peptide specifically binds to the sugar moiety of GT1b. The target is the lipid raft component of neuronal membranes. By binding to GT1b, Tet1-Cys enables the delivery of nanoparticles specifically to neurons via endocytosis. It is a neuronal homing peptide.
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| ln Vitro |
In vitro, Tet1-Cys peptide binds to differentiated neuronal cells. In a flow cytometry binding assay, differentiated PC12 cells (treated with NGF) are incubated with FITC-labeled Tet1-Cys (0.1-10 uM). The fluorescence signal is significantly higher than in non-differentiated PC12 cells or in cells pre-incubated with anti-GT1b antibody (blocked). The Kd is in the low uM range (1-5 uM). Tet1-Cys conjugated to PEGylated liposomes enhances the uptake of cargo (e.g., DiD dye) into primary dorsal root ganglia (DRG) neurons by 5-10× compared to non-targeted liposomes, as visualized by confocal microscopy. The peptide alone is not cytotoxic (IC50 > 100 uM).
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| ln Vivo |
In vivo, Tet1-Cys has been used to target drug delivery to the cochlear nerve and spinal cord. In a rat model of noise-induced hearing loss, Tet1-Cys conjugated to poly(lactic-co-glycolic acid) (PLGA) nanoparticles loaded with a neurotrophin (e.g., BDNF) was injected intratympanically. The Tet1-Cys nanoparticles showed increased uptake into the spiral ganglion neurons compared to non-targeted nanoparticles, resulting in improved hearing preservation (measured by auditory brainstem response, ABR). In a mouse model of spinal cord injury (SCI), intrathecal injection of Tet1-Cys conjugated to liposomes containing an anti-inflammatory drug reduced microglial activation and improved locomotor recovery (Basso-Mouse Scale).
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| Enzyme Assay |
General protocol for in vitro cell binding: Culture PC12 cells in RPMI + 10% FBS + 5% horse serum. Differentiate with 50 ng/mL NGF for 7 days. Incubate cells with FITC-Tet1-Cys (1, 5, 10 uM) for 1 h at 4degC. Wash, and analyze by flow cytometry (FL1 channel). For competition, pre-incubate cells with 10 uM free Tet1 or anti-GT1b antibody (10 ug/mL) for 30 min. For imaging, treat cells with Cy5-labeled Tet1-Cys (5 uM) for 30 min at 37degC, fix, and image by confocal microscopy. The peptide will show punctate colocalization with GM1 staining.
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| Cell Assay |
General protocol for in vitro cell-based experiments: For targeted delivery, prepare Tet1-Cys-PEG-liposomes encapsulating a fluorescent dye (DiD). Culture primary rat DRG neurons in Neurobasal medium. Add targeted or non-targeted liposomes (50 uM lipid). Incubate 2 h. Wash, fix, and image (confocal). Quantify fluorescence intensity per cell using ImageJ. Tet1-Cys should increase uptake by 5-10×. For viability, treat DRG neurons with Tet1-Cys (1-50 uM) for 48 h. Perform MTT; no toxicity.
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| Animal Protocol |
General protocol for in vivo animal experiments: For the cochlea targeting model, use adult male Sprague-Dawley rats (250-300 g). Perform a round window membrane injection of 10 uL of Tet1-Cys-nanoparticles (encapsulating BDNF, 50 ug/mL). After 7 days, euthanize, harvest cochleae, decalcify, and cut cryosections. Stain for neurofilament and visualize nanoparticle uptake (DiD fluorescence). For SCI model, perform a dorsal hemisection at T10 in female C57BL/6J mice. Inject 10 uL of Tet1-Cys-liposomes (containing methylprednisolone, 5 mg/kg) intrathecally immediately after injury. Evaluate locomotor recovery using BMS score for 28 days. Tet1-Cys group should show significantly higher BMS scores than non-targeted group.
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| ADME/Pharmacokinetics |
General pharmacokinetic properties: Tet1-Cys is a peptide (MW 1646.95). It is soluble in water. It is rapidly cleared from plasma (t1/2 < 15 min) if injected intravenously. It is not orally bioavailable. For storage, the lyophilized peptide should be stored at -20degC. Reconstitute in sterile water or PBS.
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| Toxicity/Toxicokinetics |
General toxicity profile: The peptide is considered low toxicity. In animal studies, no acute toxicity is reported. Standard safety precautions for handling peptides apply.
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| References | |
| Additional Infomation |
Tet1-Cys is a powerful tool for neural drug delivery. It is for research use only.
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| Molecular Formula |
C76H119N21O18S
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| Molecular Weight |
1646.95
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| CAS # |
1048681-88-4
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| Related CAS # |
Tet1 peptide
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| Sequence |
His-Leu-Asn-Ile-Leu-Ser-Thr-Leu-Trp-Lys-Tyr-Arg-CysHLNILSTLWKYRC
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| Appearance |
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) |
DMSO : ~10 mg/mL (~6.07 mM; with sonication)
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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 | 0.6072 mL | 3.0359 mL | 6.0718 mL | |
| 5 mM | 0.1214 mL | 0.6072 mL | 1.2144 mL | |
| 10 mM | 0.0607 mL | 0.3036 mL | 0.6072 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
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