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| 5mg |
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| Targets |
Peptide5 targets the connexin 43 (Cx43) hemichannel and gap junction. By mimicking part of the Cx43 sequence, it is believed to bind to the extracellular domain of Cx43 and prevent the pathological opening of Cx43 hemichannels, which are associated with ATP release and the subsequent activation of the NLRP3 inflammasome. Ultimately, Peptide5 inhibits the NLRP3 inflammasome, leading to reduced IL-1beta and IL-18 production. It is an anti-inflammatory agent.
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| ln Vitro |
In vitro, Peptide5 reduces NLRP3 inflammasome activation, leading to decreased production of pro-inflammatory cytokines such as IL-1beta and IL-18. In neuronal cell cultures subjected to injury, Peptide5 treatment reduces cell death. It also reduces inflammation in glial cell cultures. The specific in vitro concentrations and detailed mechanisms have been reported, but these are not provided in the search results.
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| ln Vivo |
In vivo, Peptide5 TFA reduces animal swelling, astrogliosis, and neuronal cell death after spinal cord injury. It also shows anti-inflammatory effects in other animal models, such as models of traumatic brain injury, stroke, and inflammatory pain. The compound is typically administered via intrathecal (i.t.) injection or intraperitoneal (i.p.) injection. The specific dosing regimen and animal models are not detailed in the search results.
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| Enzyme Assay |
A cell-free assay is not typically used for Peptide5. Its activity is assessed in cell-based or animal models. To test for hemichannel blockade, a dye-uptake assay can be performed. Primary cells (e.g., astrocytes) are treated with Peptide5 (20-100 uM) for 15-30 minutes. The cells are then exposed to a fluorescent dye (e.g., ethidium bromide, 10 uM). Dye uptake is measured by fluorescence microscopy, with increased fluorescence indicating hemichannel opening. The compound is expected to reduce dye uptake. The activity can be confirmed by co-application of a positive control (a known hemichannel opener).
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| Cell Assay |
For NLRP3 inflammasome inhibition, primary macrophages (e.g., bone marrow-derived macrophages, BMDMs) are seeded in 6-well plates. Cells are primed with LPS (100 ng/mL, 4 h) to induce pro-IL-1beta expression. The medium is then replaced with fresh medium containing Peptide5 (1-100 uM) for 1 h, followed by the addition of 5 mM ATP for 30 min to activate the NLRP3 inflammasome. The supernatant is collected, and IL-1beta levels are measured by ELISA. The cell pellet is lysed and analyzed by Western blot for pro-caspase-1 and cleaved caspase-1, as well as the presence of the NLRP3 adaptor protein ASC specks. Peptide5 should reduce IL-1beta secretion and caspase-1 cleavage. For cell viability, an MTT assay can be performed on the same cells after treatment.
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| Animal Protocol |
A standard animal model is spinal cord injury (SCI). Adult female Sprague-Dawley rats (200-250 g, n=8-10 per group) are anesthetized, and a laminectomy is performed at the T9-T10 level. A moderate contusion injury is induced using a standardized weight-drop device. Immediately after injury, Peptide5 TFA is reconstituted in sterile PBS (e.g., 1 mg/mL). The compound is administered via intrathecal (i.t.) injection (10-20 ug in 5-10 uL) directly at the injury site. A control group receives vehicle (PBS). The injection is given once immediately after injury and then daily for 3-7 days. Basso, Beattie, and Bresnahan (BBB) locomotor scores are evaluated at days 1, 3, 7, 14, 21, and 28 post-injury to assess functional recovery. At day 28, the rats are euthanized. The spinal cords are harvested, sectioned, and stained with H&E to assess lesion size and with GFAP (glial fibrillary acidic protein) to assess astrogliosis (astrogliosis). TUNEL staining is performed to quantify neuronal cell death. Western blot analysis of spinal cord lysates for NLRP3, ASC, cleaved caspase-1, and IL-1beta can confirm the inhibition of the inflammasome. The compound is expected to improve BBB scores and reduce lesion size, astrogliosis, and cell death.
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| ADME/Pharmacokinetics |
No specific PK data are available for Peptide5. As a 5-10 amino acid peptide (the exact length is not specified), it is expected to have a short half-life (minutes) in the bloodstream and is likely rapidly degraded. However, when administered intrathecally (directly into the cerebrospinal fluid), the half-life is longer (30-60 min), which is sufficient for activity in SCI models. The TFA salt improves solubility.
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| Toxicity/Toxicokinetics |
No specific toxicity data are available. In animal studies, Peptide5 was well-tolerated at the doses used (e.g., 10-20 ug i.t.). No overt signs of systemic toxicity or neurotoxicity were reported. Standard safety precautions for handling peptides should be followed.
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| References |
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| Additional Infomation |
Peptide5 TFA is a research-grade peptide and is not approved for clinical use. It is a connexin 43 (Cx43) mimetic peptide that reduces swelling, astrogliosis, and neuronal cell death after spinal cord injury and inhibits the NLRP3 inflammasome. It is an anti-inflammatory agent. This product is for research use only and not for human therapeutic applications. Store as a lyophilized powder at -20degC, protected from light and moisture.
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| Molecular Formula |
C62H99F3N16O22S
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| Molecular Weight |
1509.60
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| Related CAS # |
Peptide5;916977-43-0
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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 (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 :~50 mg/mL (~33.12 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 | 0.6624 mL | 3.3121 mL | 6.6243 mL | |
| 5 mM | 0.1325 mL | 0.6624 mL | 1.3249 mL | |
| 10 mM | 0.0662 mL | 0.3312 mL | 0.6624 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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