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| Targets |
The primary target of CALP3 is calmodulin (CaM), a Ca2+-binding messenger protein that transduces Ca2+ signals by activating various target enzymes. CALP3 binds to the EF-hand Ca2+-binding site on calmodulin, activating it even in the absence of Ca2+. By directly binding to calmodulin, CALP3 mimics elevated intracellular Ca2+ and regulates Ca2+ channels and pumps. This mechanism allows CALP3 to bypass normal Ca2+ signaling pathways and directly modulate calmodulin-dependent processes.
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| ln Vitro |
Glutamate-induced substantial and sustained increase in [Ca2+]i is inhibited in a dose-dependent manner (IC50=37.25 μM) by CALP3 (50, 100, 150, 200 μM) in neuronal cells loaded with Fura-2 [1]. In cultured rat neocortical neurons, CALP3 (50, 100, 150, and 200 μM) reduces glutamate-induced cytotoxicity in a dose-dependent manner (IC50=50.97 μM). Apoptosis is dose-dependently inhibited by CALP3 (IC50 = 33.41 μM) [1]. Human T cell apoptosis mediated by HIV gp120 and SAg is inhibited by CALP3 (100 μM) [1]. Gossypol-induced necrosis is decreased and the percentage of viable cells is increased by CALP3 (100 μM; 15 min pretreatment) [2]. Fmoc-Asp(PEG-PS)-OA1 was the starting point for the synthesis of Cyclic-CALP3. Ca21 inflow was not inhibited by cyclic CALP3, and this peptide was used as a negative control. Glutamate's actions are not inhibited by cyclic CALP3 [1].
In vitro, CALP3 (50, 100, 150, and 200 uM) reduces glutamate-induced cytotoxicity in cultured rat neocortical neurons in a dose-dependent manner (IC₅0 = 50.97 uM). It inhibits glutamate-caused large sustained increases in [Ca2+]i. CALP3 activates phosphodiesterase in the absence of Ca2+ and inhibits Ca2+-mediated cytotoxicity and apoptosis (IC₅0 = 33 microM). It also decreases gossypol-induced necrosis and increases live cell fraction. The compound acts as a potent Ca2+ channel blocker and targets the calcium channel pathway. |
| ln Vivo |
In vivo, CALP3 has been investigated for its potential in controlling apoptosis in conditions such as AIDS or neuronal loss due to ischemia. While detailed animal model studies are limited, its ability to modulate Ca2+ signaling suggests applications in neurodegenerative disease models. CALP3 can be formulated for in vivo administration using 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline or 10% DMSO + 90% (20% SBE-beta-CD in Saline), yielding clear solutions at ≥ 1.25 mg/mL (1.42 mM). Further in vivo studies are required to fully establish efficacy and safety.
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| Enzyme Assay |
For calmodulin binding assays, use fluorescently labeled calmodulin or a calmodulin-dependent phosphodiesterase (PDE) activity assay. Incubate purified calmodulin (50-100 nM) with increasing concentrations of CALP3 (0.1-100 uM) in binding buffer (50 mM Tris-HCl pH 7.5, 100 mM KCl, 1 mM MgCl2, 0.1 mM CaCl2) for 15-30 min at room temperature. For PDE activation assays, add calmodulin (10 nM), PDE (10 ng/mL), and [3H]-cAMP or colorimetric substrate, incubate for 20 min at 30degC, then terminate and measure PDE activity using scintillation counting or absorbance. Calculate EC₅0 values for calmodulin activation.
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| Cell Assay |
Culture rat neocortical neurons or other neuronal cell lines (e.g., SH-SY5Y, PC12) in neurobasal medium with B27 supplement at 37degC with 5% CO2. For cytotoxicity assays, treat cells with CALP3 (12.5-200 uM) for 1 hour, then expose to glutamate (100 uM) for 24 hours to induce excitotoxicity. Assess cell viability using MTT assay, LDH release, or propidium iodide staining. For apoptosis studies, incubate cells with CALP3 (25-100 uM) for 24-48 hours and measure caspase-3/7 activity using fluorogenic substrates, or assess mitochondrial membrane potential using JC-1 dye. Evaluate protection against necrosis by co-treatment with gossypol (10 uM) and CALP3 (1-50 uM) for 24 hours.
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| Animal Protocol |
For in vivo studies, use male C57BL/6 mice (8-12 weeks, 20-25 g) or Sprague-Dawley rats (200-300 g) in models of ischemia or neurodegeneration. Administer CALP3 via intraperitoneal (i.p.) injection at doses ranging from 1-30 mg/kg, formulated in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline to achieve a clear solution at ≥ 1.25 mg/mL. For acute studies, administer CALP 30-60 min before inducing ischemia (e.g., middle cerebral artery occlusion) or neurotoxin exposure (e.g., MPTP or 6-OHDA). Monitor neurological scores, body weight daily, and assess brain tissue at 24-72 h post-insult for infarct volume (TTC staining) and markers of apoptosis (TUNEL, cleaved caspase-3).
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| ADME/Pharmacokinetics |
CALP3 has a molecular formula of C44H₆₈N10O₉ and a molecular weight of 881.07 g/mol. Solubility in DMSO is ~12.5 mg/mL (~14.19 mM) and in water is 1 mg/mL (1.13 mM). For in vivo use, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline or 10% DMSO + 90% (20% SBE-beta-CD in Saline). The compound should be stored as a powder at -20degC for up to 3 years and in solvent at -80degC for 1 year. It is classified as a solid powder and should be stored in a sealed, moisture-protected environment.
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| Toxicity/Toxicokinetics |
Based on its peptide nature and mechanism of action, CALP3 is expected to have low acute toxicity at typical research concentrations. Standard laboratory precautions should be followed: use personal protective equipment including gloves and lab coat, avoid inhalation and skin contact. The compound is for research use only and not intended for therapeutic use in humans. No specific teratogenic, mutagenic, or carcinogenic effects have been reported for this compound. Consult the safety data sheet before handling. Dispose of waste according to local regulations for chemical and biological waste.
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| References |
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| Additional Infomation |
CALP3 is a research tool peptide used exclusively for in vitro and in vivo studies of calmodulin-mediated signaling, Ca2+ homeostasis, and apoptosis regulation. Its primary applications include: 1) Studying calmodulin-dependent processes such as phosphodiesterase activation; 2) Investigating neuroprotective mechanisms against excitotoxicity and oxidative stress; 3) Exploring apoptosis pathways in neuronal degeneration and ischemia; 4) As a tool compound for dissecting Ca2+ signaling cascades. It has no approved clinical use. The peptide sequence is VKFGVGFK.
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| Molecular Formula |
C₄₄H₆₈N₁₀O₉
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| Molecular Weight |
881.07
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| Exact Mass |
880.517
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| CAS # |
261969-05-5
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| PubChem CID |
10033623
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| Appearance |
White to off-white solid powder
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| LogP |
3.947
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
29
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| Heavy Atom Count |
63
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| Complexity |
1470
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC(C)[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCC(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCCCN)C(=O)O)N
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| InChi Key |
OBMFGXCPBIYSPH-FFIZALLVSA-N
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| InChi Code |
InChI=1S/C44H68N10O9/c1-27(2)37(47)42(60)51-31(19-11-13-21-45)40(58)53-33(23-29-15-7-5-8-16-29)39(57)48-26-36(56)54-38(28(3)4)43(61)49-25-35(55)50-34(24-30-17-9-6-10-18-30)41(59)52-32(44(62)63)20-12-14-22-46/h5-10,15-18,27-28,31-34,37-38H,11-14,19-26,45-47H2,1-4H3,(H,48,57)(H,49,61)(H,50,55)(H,51,60)(H,52,59)(H,53,58)(H,54,56)(H,62,63)/t31-,32-,33-,34-,37-,38-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-amino-3-methylbutanoyl]amino]hexanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]hexanoic acid
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| Synonyms |
CALP-3; CALP 3
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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 : ~12.5 mg/mL (~14.19 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.42 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 12.5 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: ≥ 1.25 mg/mL (1.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 12.5 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: ≥ 1.25 mg/mL (1.42 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 | 1.1350 mL | 5.6749 mL | 11.3498 mL | |
| 5 mM | 0.2270 mL | 1.1350 mL | 2.2700 mL | |
| 10 mM | 0.1135 mL | 0.5675 mL | 1.1350 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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