| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary target is dynamin-related protein 1 (Drp1). P110 specifically inhibits the interaction between Drp1 and its adaptor protein Fis1 on the mitochondrial outer membrane. By blocking this protein-protein interaction, the peptide prevents the translocation of Drp1 from the cytosol to the mitochondria and inhibits its GTPase activity, thereby suppressing pathological mitochondrial fission. It displays no effect on dynamin 1 or other mitochondrial dynamics-related proteins.
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| ln Vitro |
In vitro, P110 inhibits Drp1 GTPase activity (IC50 ~2 uM) and blocks mitochondrial fragmentation in cell culture. It reduces mitochondrial dysfunction, reactive oxygen species (ROS) production, and programmed cell death. In neuronal cell models of Parkinson's disease (e.g., SH-SY5Y cells treated with MPP+), P110 (0.1-10 uM) significantly improves cell viability and preserves mitochondrial morphology, reducing the percentage of cells with fragmented mitochondria from 60% to 20%.
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| ln Vivo |
In vivo, P110 has demonstrated neuroprotective effects in multiple animal models. In a mouse model of Parkinson's disease (MPTP), intranasal administration of P110 (1 mg/kg) or intraperitoneal injection (1 mg/kg) before each MPTP injection reduced dopaminergic neuron loss in the substantia nigra by >50% and ameliorated behavioral deficits. It has also shown efficacy in models of Huntington's disease, stroke, and sepsis without blocking normal cell division.
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| Enzyme Assay |
A non-cell-based GTPase activity assay is performed using recombinant Drp1 protein. Drp1 (100 nM) is incubated with GTP (200 uM) in assay buffer (20 mM HEPES, 2 mM MgCl2, 1 mM DTT, pH 7.5) with varying concentrations of P110 (0.1-100 uM) at 37degC for 30 minutes. The inorganic phosphate released is detected using a malachite green reagent, and absorbance at 620 nm is measured. The IC50 for GTPase inhibition is calculated. For direct binding, surface plasmon resonance (SPR) can be used.
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| Cell Assay |
In a typical cell-based assay, primary rat cortical neurons or SH-SY5Y cells are pre-treated with P110 (1-10 uM) for 1 hour. They are then exposed to an apoptotic stimulus (e.g., 1 uM staurosporine, 500 uM MPP+, or oxygen-glucose deprivation). After 24 hours, mitochondrial morphology is visualized by staining with MitoTracker Red (100 nM, 30 min) and confocal microscopy. Cells with fragmented mitochondria are counted. Cell viability is measured by MTT assay, and LDH release is measured to quantify cell death. ROS production is measured using DCFH-DA.
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| Animal Protocol |
A standard in vivo protocol for Parkinson's disease uses male C57BL/6 mice (8-10 weeks). MPTP (20 mg/kg, 4 injections, 2 hours apart) is administered intraperitoneally. P110 TFA is dissolved in sterile saline (1 mg/mL) and administered intranasally (10 uL per nostril, 1 mg/kg) or intraperitoneally (1 mg/kg) 1 hour before each MPTP injection. For chronic infusion, an osmotic minipump is implanted into the lateral ventricle (0.5 uL/h, 0.5 mg/mL). Mice are euthanized 7 days later. Brain sections are immunostained for tyrosine hydroxylase (TH) to count dopaminergic neurons in the substantia nigra. Striatal dopamine and its metabolites are measured by HPLC.
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| ADME/Pharmacokinetics |
As a TAT-conjugated peptide (MW ~2525 Da), P110 is cell-permeable and can cross the blood-brain barrier to some extent, especially when administered intranasally. Its half-life in plasma is short (likely minutes) due to rapid proteolytic degradation, which is why in vivo studies require repeated injections or continuous infusion. The peptide is cleared renally and catabolized into amino acids. Formulation in sterile saline or DMSO/saline is typical. Plasma protein binding is low.
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| Toxicity/Toxicokinetics |
Toxicity data for P110 in animals is not extensively published, but studies indicate it is well-tolerated at neuroprotective doses (1 mg/kg IP). The compound does not block the physiological functions of Drp1 required for cell division, suggesting a selective effect on pathological fission. The TAT peptide carrier is generally considered safe. However, repeated administration of foreign peptides can potentially elicit an immune response in some animal models. Acute toxicity studies are typically performed by the manufacturer.
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| References | |
| Additional Infomation |
P110 TFA is a research tool peptide and not an FDA-approved drug. It is widely used in cell biology and neuroscience to study the role of mitochondrial dynamics in disease. The peptide sequence is derived from the Drp1 binding site on Fis1 and is conjugated to a TAT sequence (YGRKKRRQRRR) to facilitate cell entry. While highly effective in research models, its clinical development is limited by its peptide nature (poor oral bioavailability, rapid degradation, potential immunogenicity). It serves as a valuable tool for validating Drp1 as a therapeutic target for diseases such as Parkinson's, Alzheimer's, Huntington's, stroke, and cardiomyopathy.
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| Molecular Formula |
C100H179N45O25.XC2HF3O2
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| Molecular Weight |
2411.78 (free base)
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| Related CAS # |
Drp1 peptide inhibitor P110
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| Sequence |
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Gly-Gly-Asp-Leu-Leu-Pro-Arg-Gly-Ser-NH2YGRKKRRQRRRGGDLLPRGS-NH2
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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) |
DMSO : ≥ 100 mg/mL
H2O : ~20 mg/mL (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.) |
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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