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| Targets |
Calcineurin substrate TFA targets calcineurin (Ca2+/calmodulin-dependent protein phosphatase, also known as PP2B), a conserved serine/threonine phosphatase. It functions as an enzyme substrate rather than a pharmacologically active drug. After being phosphorylated at the serine residue by PKA, the phosphorylated peptide can be used for the detection of calcineurin activity. This allows for the measurement of calcineurin-mediated dephosphorylation, which is involved in T cell activation, cardiac hypertrophy, and synaptic plasticity.
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| ln Vitro |
In vitro, calcineurin substrate TFA is a substrate for calcineurin, and its phosphorylated form is used to detect calcineurin activity in biochemical assays. It is not typically used in cell viability or proliferation assays, as it is a biochemical reagent rather than a modulator of biological activity. The peptide sequence is derived from the regulatory RII subunit of PKA and contains the specific phosphorylation site (Ser) recognized by PKA and dephosphorylation site recognized by calcineurin.
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| ln Vivo |
In vivo activity data for calcineurin substrate TFA are not applicable, as the compound is a biochemical substrate used in cell-free activity assays. It is not designed for in vivo administration as a therapeutic agent, and no animal efficacy or pharmacokinetic studies are standard for this type of substrate peptide. It is strictly a research tool for enzymatic studies.
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| Enzyme Assay |
The phosphorylated form of calcineurin substrate TFA is used in non-cellular assays to measure calcineurin phosphatase activity. The protocol involves incubating purified calcineurin enzyme with various concentrations of the phosphorylated peptide substrate in a reaction buffer containing Ca2+, calmodulin, and Ni2+. The reaction is allowed to proceed, and the release of free phosphate is quantified using a malachite green-based colorimetric detection kit, or the amount of remaining phosphorylated peptide is measured by HPLC or MS.
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| Cell Assay |
Calcineurin substrate TFA is not used for cell-based functional assays as an active modulator. For analytical applications, the peptide can be used to assess calcineurin activity in cell lysates. Cells are lysed, and the lysate is incubated with the phosphorylated version of calcineurin substrate TFA in the presence of Ca2+ and calmodulin. The dephosphorylation reaction is stopped, and the amount of phosphate released is quantified colorimetrically. This allows for the measurement of endogenous calcineurin activity in cellular samples.
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| Animal Protocol |
In vivo animal experiments are not conducted with calcineurin substrate TFA, as it is a biochemical tool for in vitro assays. There are no animal models or administration protocols described for this substrate peptide in standard product literature. The compound is strictly used for enzymatic activity measurements in lysates or purified systems.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for calcineurin substrate TFA are not available or applicable. This compound is a peptide substrate used for in vitro biochemical assays to measure calcineurin enzyme activity. It is not designed or characterized for in vivo administration, and no ADME (absorption, distribution, metabolism, excretion) data are provided in standard product literature.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for calcineurin substrate TFA are not reported in standard product literature. As a research-use peptide substrate, standard safety assessments for acute toxicity, genotoxicity, and organ-specific toxicity are not typically described. For laboratory use, standard chemical safety precautions for handling peptides should be followed. The compound is generally considered non-hazardous at the concentrations used in biochemical assays.
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| References |
[1]. Crabtree GR, et al. Calcium, calcineurin, and the control of transcription. J Biol Chem. 2001 Jan 26;276(4):2313-6.
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| Additional Infomation |
Calcineurin substrate TFA (PKA RII peptide TFA) is a synthetic peptide that is a substrate for calcineurin. The exact sequence and molecular weight are not detailed in the search results. The peptide is derived from the regulatory RII subunit of cAMP-dependent protein kinase (PKA). It is typically stored at -20degC, protected from moisture. The product is for research use only and is used as a positive control in calcineurin activity assays.
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| Molecular Formula |
C94H151F3N28O31
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| Molecular Weight |
2226.37
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| Related CAS # |
Calcineurin substrate;113873-67-9
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| Appearance |
Typically exists as solid at room temperature
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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) |
H2O :~25 mg/mL (~11.23 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 | 0.4492 mL | 2.2458 mL | 4.4916 mL | |
| 5 mM | 0.0898 mL | 0.4492 mL | 0.8983 mL | |
| 10 mM | 0.0449 mL | 0.2246 mL | 0.4492 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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