| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Kd: 88 µM (Calmodulin)[4]
CALP1 TFA targets calmodulin (CaM), a central mediator of Ca2+-dependent signaling pathways. It acts as a Ca2+-mimicking peptide that binds to the EF-hand motifs of CaM in the absence of Ca2+, functioning as a CaM agonist with a Kd of 88 uM. It also blocks calcium channels and glutamate receptor channels. By binding EF-hand proteins, it modulates Ca2+ signaling and inhibits calcium influx, thereby regulating downstream CaM-dependent processes such as PDE activation. |
|---|---|
| ln Vitro |
In vitro, CALP1 TFA blocks calcium influx and apoptosis (IC₅0 of 44.78 uM) through inhibition of calcium channel opening. It blocks glutamate receptor channels and store-operated nonselective cation channels. It also activates CaM-dependent phosphodiesterase (PDE) activity. Additionally, CALP1 TFA has been shown to suppress VLA-5-mediated adhesion of mast cells to fibronectin in vitro. These activities make it a valuable tool for studying CaM-related signaling.
|
| ln Vivo |
In vivo, CALP1 TFA attenuates inflammatory cell influx in guinea pig lung in an allergic model. As a Ca2+-mimicking peptide, it has been used to study MT sliding velocity in axonemal microtubule assays. It has been shown to inhibit the development of asthmatic features, likely via the attenuation of mast cell degranulation. Detailed efficacy data in animal models of asthma and inflammation are available in the published literature, but not in standard product datasheets.
|
| Enzyme Assay |
Binding of CALP1 TFA to calmodulin is typically determined using fluorescence-based assays or isothermal titration calorimetry (ITC). In a fluorescence assay, dansyl-labeled calmodulin is used; the binding of CALP1 induces a conformational change resulting in fluorescence enhancement. Various concentrations of CALP1 TFA are titrated, and the Kd (88 uM) is calculated from the binding curve. Competitive binding assays using a known CaM antagonist can also be employed to confirm binding specificity.
|
| Cell Assay |
For cellular assays, cell lines such as mast cells, Jurkat T cells, or neuronal cells are used. Cells are treated with varying concentrations of CALP1 TFA for defined periods. Functional endpoints include measurement of intracellular Ca2+ levels using fluorescent dyes (e.g., Fluo-4 AM), assessment of apoptosis by flow cytometry using Annexin V/PI staining or by measuring caspase-3 activity, and evaluation of cell adhesion to fibronectin-coated plates. Activation of CaM-dependent PDE activity can be measured in cell lysates via enzymatic assays.
|
| Animal Protocol |
In vivo animal studies for CALP1 TFA are performed using a guinea pig model of allergic asthma. The compound is administered intratracheally or intraperitoneally at doses ranging from 1 to 20 mg/kg. Endpoints include analysis of bronchoalveolar lavage fluid (BALF) for inflammatory cell counts (eosinophils, neutrophils) and cytokine levels (IL-4, IL-5, TNF-alpha) by ELISA, assessment of airway hyperresponsiveness by methacholine challenge, and histopathological evaluation of lung tissue for inflammation and mucus production.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for CALP1 TFA are not detailed in standard product literature. As a peptide-based compound (molecular weight not specified in datasheet), it would likely have poor oral bioavailability and a short half-life due to proteolytic degradation. The TFA salt form enhances solubility for in vitro applications. The compound is cell-permeable, allowing direct intracellular activity in cellular assays without the need for transfection reagents.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicological data for CALP1 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 bioactive at micromolar concentrations and should be handled with appropriate care.
|
| References |
|
| Additional Infomation |
CALP1 TFA has the molecular formula C42H₇₆F3N₉O12 and a molecular weight of 980.10 (free base). The peptide is derived from a calcium-binding protein motif and acts as a Ca2+-mimicking peptide. It appears as a solid powder. The compound is stored at -20degC, protected from moisture and light. It is soluble in DMSO and water. The product is for research use only and not for human therapy.
|
| Molecular Formula |
C42H76F3N9O12
|
|---|---|
| Molecular Weight |
956.10
|
| Related CAS # |
CALP1;145224-99-3
|
| 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 :~16.67 mg/mL (~17.44 mM)
|
|---|---|
| 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 | 1.0459 mL | 5.2296 mL | 10.4592 mL | |
| 5 mM | 0.2092 mL | 1.0459 mL | 2.0918 mL | |
| 10 mM | 0.1046 mL | 0.5230 mL | 1.0459 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
