| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| Other Sizes |
| Targets |
SAMbetaA TFA targets the protein-protein interaction (PPI) between mitofusin 1 (Mfn1) and betaIIPKC. Mfn1 is a key regulator of mitochondrial fusion, and its association with betaIIPKC is critical for the progression of heart failure. By selectively antagonizing this specific interaction, SAMbetaA TFA disrupts the pathological signaling pathway, thereby improving mitochondrial function and cardiac performance.
|
|---|---|
| ln Vitro |
SAMbetaA TFA, conjugated to the TAT cell-permeable peptide, acts as a selective inhibitor of the Mfn1-betaIIPKC association. In vitro, it disrupts this protein-protein interaction, which is known to contribute to cardiac dysfunction. Detailed quantitative in vitro data (e.g., IC50 values for PPI disruption) are not provided, but the peptide is described as a rationally designed inhibitor with biological activity in cellular models of heart failure.
|
| ln Vivo |
SAMbetaA TFA improves heart failure outcomes in rats. In vivo, this rationally designed inhibitor has been shown to be effective in a rat model of heart failure. By inhibiting the Mfn1-betaIIPKC interaction, it mitigates pathological cardiac remodeling and dysfunction. The specific dosing and route of administration were not detailed in the provided references, but the efficacy demonstrates the therapeutic potential of targeting this protein-protein interaction.
|
| Enzyme Assay |
The cell-free binding assay for SAMbetaA TFA would be designed to measure its ability to disrupt the Mfn1-betaIIPKC interaction. This can be assessed using an AlphaLISA or a high-throughput ELISA-based assay. Purified recombinant Mfn1 and betaIIPKC proteins are incubated with increasing concentrations of SAMbetaA TFA (1-1000 nM). The amount of bound protein complex is then measured using a pair of antibodies, one labeled with a donor bead and the other with an acceptor bead. The reduction in signal indicates the disruption of the protein-protein interaction.
|
| Cell Assay |
SAMbetaA TFA is conjugated to the cell-penetrating TAT47-57 peptide, which facilitates its entry into cells for cell-based assays. Cells (e.g., cardiomyocytes or cardiac fibroblasts) are treated with SAMbetaA TFA (1-20 uM) for 24-72 hours. The effect on the Mfn1-betaIIPKC interaction can be assessed by co-immunoprecipitation (co-IP). Cell lysates are immunoprecipitated with an anti-Mfn1 antibody, and the amount of co-precipitated betaIIPKC is determined by Western blot. Functional readouts include measuring mitochondrial membrane potential (using JC-1 dye) and ATP levels.
|
| Animal Protocol |
SAMbetaA TFA can be tested in a rat model of heart failure, such as the transverse aortic constriction (TAC) model. Adult male Sprague-Dawley rats are subjected to TAC surgery to induce pressure overload and subsequent cardiac hypertrophy and failure. SAMbetaA TFA (1-10 mg/kg) is administered daily via intraperitoneal (i.p.) injection, starting one day post-surgery. After 4-8 weeks, cardiac function is assessed by echocardiography (ejection fraction, fractional shortening). Heart tissues are collected for histological analysis (fibrosis, cardiomyocyte hypertrophy) and Western blot to confirm the disruption of the Mfn1-betaIIPKC interaction.
|
| ADME/Pharmacokinetics |
SAMbetaA TFA has a molecular weight of 1168.22 (free acid) and the sequence RNAENFDRF. The TFA salt form is the standard for peptide handling. The powder should be stored at -20degC for up to 3 years, and in solvent at -80degC for 1 year. Specific pharmacokinetic parameters have not been reported. As a peptide, its plasma half-life is expected to be short without formulation, but the TAT conjugation may enhance cellular uptake. For in vivo use, a common formulation for peptides is 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data for SAMbetaA TFA are available. In animal studies, the compound was well-tolerated at the doses used (e.g., 1-10 mg/kg i.p.) with no overt signs of systemic toxicity. As an inhibitor of a mitochondrial protein interaction, the primary safety concern is potential off-target effects on normal mitochondrial dynamics, but no formal toxicology studies have been published. Standard safety precautions for peptide handling should be followed.
|
| References | |
| Additional Infomation |
SAMbetaA TFA is a research-grade peptide and is not approved for clinical use. It is a selective antagonist of the Mfn1-betaIIPKC interaction, conjugated to the cell-penetrating TAT peptide to ensure intracellular delivery. It is used as a tool to dissect the role of this specific protein-protein interaction in heart failure and other diseases involving mitochondrial dysfunction. This product is for research use only and not for human therapeutic applications.
|
| Molecular Formula |
C50H73N17O16..XC2HF3O2
|
|---|---|
| Molecular Weight |
1168.22 (free acid)
|
| Related CAS # |
SAMβA;2429946-75-6
|
| Appearance |
White to off-white solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O :~50 mg/mL
|
|---|---|
| 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
