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| 1mg |
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| Other Sizes |
| Targets |
IIQLPEIVVV TFA targets the protein-protein interaction between Drp1 (dynamin-related protein 1) and Mff (mitochondrial fission factor). Drp1 is a large GTPase that mediates mitochondrial fission, and Mff is a receptor on the mitochondrial outer membrane that recruits Drp1. By specifically inhibiting this interaction, the peptide blocks the recruitment of Drp1 to mitochondria, thereby preventing physiological (but not pathological) fission, ultimately leading to mitochondrial dysfunction.
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| ln Vitro |
IIQLPEIVVV TFA is a specific inhibitor of the Drp1-Mff interaction. It discriminates between physiological and pathological fission, hindering physiological fission which leads to mitochondrial dysfunction. While specific IC50 values are not provided, its inhibitory activity is demonstrated by the disruption of Drp1 localization to mitochondria. It is used in Huntington‘s disease research, indicating its utility in studying mitochondrial dynamics in neurodegeneration.
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| ln Vivo |
Specific in vivo activity data for IIQLPEIVVV TFA is not provided. However, it is utilized in research related to Huntington‘s disease, suggesting its application in animal models of this disorder. By inhibiting the Drp1-Mff interaction, the peptide may influence mitochondrial morphology and function in vivo, potentially affecting disease progression. Further studies are required to establish its in vivo efficacy.
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| Enzyme Assay |
The binding of IIQLPEIVVV TFA to Drp1 or Mff can be assessed by surface plasmon resonance (SPR) or biolayer interferometry (BLI). Procedure: Recombinant Drp1 or Mff protein is immobilized on a biosensor chip. Varying concentrations of IIQLPEIVVV TFA (0.1-1000 nM) are injected over the chip. Association and dissociation rates are recorded, and the equilibrium dissociation constant (KD) is calculated using a 1:1 binding model. Alternatively, a fluorescence polarization (FP) competition assay using labeled Mff peptide and recombinant Drp1 can be used.
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| Cell Assay |
The cellular activity can be assessed in cell lines expressing fluorescently labeled mitochondria. Procedure: HeLa or COS-7 cells are transfected with a mitochondrial marker (e.g., Mito-DsRed). After 24 hours, cells are treated with varying concentrations of IIQLPEIVVV TFA (1-50 uM) for 4-24 hours. Cells are fixed with 4% paraformaldehyde and imaged by confocal microscopy. Mitochondrial morphology is quantified using ImageJ with the MiNA (Mitochondrial Network Analysis) macro. A reduction in mitochondrial network connectivity and an increase in fragmentation indicates inhibition of Drp1-Mff interaction and disruption of physiological fission.
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| Animal Protocol |
In vivo efficacy can be evaluated in a mouse model of Huntington‘s disease (e.g., R6/2 transgenic mice). Procedure: R6/2 mice (4 weeks old, n=10 per group) are administered IIQLPEIVVV TFA via intracerebroventricular (ICV) injection using an osmotic mini-pump at doses of 10, 30, and 100 ug/day for 4 weeks. Motor function is assessed weekly using the rotarod test and grip strength measurement. At study endpoint, brains are harvested for histological analysis of striatal neurons and for assessment of mitochondrial morphology by electron microscopy. Improvements in motor function and preservation of mitochondrial structure indicate efficacy.
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| ADME/Pharmacokinetics |
Specific PK data for IIQLPEIVVV TFA is not provided. As a 10-amino acid peptide, it is not orally bioavailable and is rapidly degraded by proteases in the circulation. For in vivo studies, it is typically administered via intracerebroventricular (ICV) injection to bypass the blood-brain barrier and achieve CNS exposure. The TFA salt improves solubility for formulation in aqueous buffers. It is stored as a powder at -20degC.
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| Toxicity/Toxicokinetics |
Specific toxicology data for IIQLPEIVVV TFA is not provided. As a peptide inhibitor of mitochondrial fission, potential on-target toxicity may include effects on cells with high metabolic demands, such as neurons and cardiomyocytes. The compound is for research use only and is not intended for human therapeutic use. Standard safety precautions for handling peptides should be followed.
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| References | |
| Additional Infomation |
IIQLPEIVVV TFA is a specific inhibitor targeting the Drp1-Mff interaction, a key protein-protein interaction in mitochondrial fission. It discriminates between physiological and pathological fission, hindering physiological fission which leads to mitochondrial dysfunction. It is used in research related to Huntington's disease and other neurodegenerative disorders where mitochondrial dynamics are dysregulated. The peptide is stored as a powder at -20degC. It is for research use only and is not an approved drug.
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| Molecular Formula |
C54H95N11O14.XC2HF3O2
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| Molecular Weight |
1122.40 (free base)
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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: (1). 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.) |
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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