| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CALP2 TFA targets calmodulin (CaM), a ubiquitous Ca2+-binding messenger protein that regulates numerous cellular processes. It binds to the CaM EF-hand/Ca2+-binding site with a Kd of 7.9 uM. By occupying the EF-hand motifs, CALP2 TFA acts as a CaM antagonist, blocking CaM-dependent signaling pathways, including phosphodiesterase activation. This makes it a valuable tool for dissecting the role of the Ca2+-sensing regulatory protein calmodulin in physiological and pathological processes.
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| ln Vitro |
In vitro, CALP2 TFA inhibits CaM-dependent phosphodiesterase activity, which increases intracellular Ca2+ concentrations as a functional consequence of CaM antagonism. It potently inhibits cell adhesion and degranulation in relevant cell types, such as mast cells. It also acts as a strong activator of alveolar macrophages. These activities make it a potent inhibitor of adhesion and degranulation, and a valuable tool for defining the role of CaM in various cellular responses.
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| ln Vivo |
Detailed in vivo activity data for CALP2 TFA are not extensively reported in standard product literature. However, as a CaM antagonist, it has been studied in allergic models. It has been shown to inhibit VLA-5-mediated adhesion of mast cells in vitro, suggesting potential for attenuating inflammatory cell influx in vivo. Further studies would be required to evaluate its efficacy in animal models of asthma, inflammation, and allergy.
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| Enzyme Assay |
Binding affinity of CALP2 TFA for calmodulin is typically determined using non-cellular assays such as fluorescence spectroscopy or isothermal titration calorimetry (ITC). In a fluorescence-based assay, dansyl-labeled calmodulin is used, and the fluorescence intensity is measured upon titration with increasing concentrations of CALP2 TFA. The Kd value is calculated from the binding curve. Alternatively, surface plasmon resonance (SPR) can be used to measure real-time binding kinetics.
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| Cell Assay |
Cellular assays for CALP2 TFA utilize various cell types, including alveolar macrophages, mast cells, or platelets. Cells are treated with varying concentrations of CALP2 TFA for defined periods. Functional endpoints include measurement of CaM-dependent phosphodiesterase (PDE) activity in cell lysates via enzymatic assays, quantification of intracellular Ca2+ levels using fluorescent dyes such as Fluo-4 AM, and assessment of degranulation by measuring the release of granular enzymes (e.g., beta-hexosaminidase) into the culture supernatant.
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| Animal Protocol |
Detailed in vivo animal protocols for CALP2 TFA are not extensively described in standard literature. A typical protocol for studying CaM antagonism in allergic inflammation could involve administering CALP2 TFA to a guinea pig model of asthma. The compound can be administered via intratracheal or intraperitoneal injection at doses of 1-10 mg/kg. Endpoints include bronchoalveolar lavage fluid (BALF) analysis for inflammatory cell counts, and histopathological analysis of lung tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for CALP2 TFA are not detailed in standard product literature. As a peptide-based calmodulin antagonist (MW 1471.72), it is not expected to be orally bioavailable and would likely have a short half-life in circulation due to proteolytic degradation. The TFA salt form is used to enhance solubility and stability for in vitro applications. For in vivo use, the compound would typically be administered via intraperitoneal or intravenous injection.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for CALP2 TFA are not detailed in standard product documentation. As a research-use compound, 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 cell-permeable and bioactive at micromolar concentrations.
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| References |
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| Additional Infomation |
CALP2 TFA has the molecular formula C₇0H10₅F3N14O1₅S and a molecular weight of 1471.72. The peptide sequence is Val-Lys-Phe-Gly-Val-Gly-Phe-Lys-Val-Met-Val-Phe (VKFGVGFKVMVF). It appears as a white to off-white solid powder. The compound is stored at -20degC or -80degC, sealed, and away from moisture. It is soluble in water and DMSO. The product is for research use only and not for human therapy.
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| Molecular Formula |
C70H105F3N14O15S
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| Molecular Weight |
1471.72
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| Related CAS # |
CALP2;261969-04-4
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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 :~50 mg/mL (~33.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (1.70 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6795 mL | 3.3974 mL | 6.7948 mL | |
| 5 mM | 0.1359 mL | 0.6795 mL | 1.3590 mL | |
| 10 mM | 0.0679 mL | 0.3397 mL | 0.6795 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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