| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Caloxin 2A1 TFA targets the plasma membrane Ca²⁺-ATPase (PMCA), inhibiting Ca²⁺-Mg²⁺-ATPase activity in human red blood cell leaky ghosts and blocking Ca²⁺-dependent formation of a 140-kDa acid-stable acylphosphate. It does not affect basal Mg²⁺-ATPase or Na⁺-K⁺-ATPase, demonstrating selectivity for PMCA.
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|---|---|
| ln Vitro |
In leaky human erythrocytes, calcoxin 2A1 TFA reduces the activity of Ca2+-Mg2+-ATPase. However, it has no effect on basal Mg2+-ATPase, Na+-K+-ATPase, or skeletal muscle sarcoplasmic reticulum Mg2+-ATPase in ghost cells. Additionally, the Ca2+-dependent synthesis of 140-kDa acid-stabilized acyl phosphates is inhibited by caloxin 2A1 TFA [1]. Airway smooth muscle cell (ASMC) apoptosis is increased by caloxin 2A1 TFA [2].
In vitro, Caloxin 2A1 TFA inhibits human red blood cell Ca²⁺-Mg²⁺-ATPase, blocking Ca²⁺-dependent formation of a 140-kDa acid-stable acylphosphate. It is a selective extracellular inhibitor of PMCA and does not affect basal Mg²⁺-ATPase or Na⁺-K⁺-ATPase. |
| ln Vivo |
Specific in vivo activity data for Caloxin 2A1 TFA are not detailed in available sources. As an inhibitor of PMCA, it may have potential for studying calcium signaling in vivo. Its extracellular mechanism of action makes it suitable for targeting cell surface PMCA.
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| Enzyme Assay |
Non-cellular enzyme assays for Caloxin 2A1 TFA involve measuring its inhibitory activity against PMCA. The compound is incubated with PMCA-containing membranes and ATP, and the inhibition of Ca²⁺-dependent ATPase activity is quantified.
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| Cell Assay |
In vitro cellular assays for Caloxin 2A1 TFA are performed using cells to assess its effects on PMCA-mediated calcium extrusion. Cells are treated with the peptide, and intracellular calcium levels are measured using fluorescent calcium indicators to evaluate PMCA inhibition.
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| Animal Protocol |
In vivo animal experiments for Caloxin 2A1 TFA would typically be conducted in animal models where PMCA function is implicated. The compound would be administered via appropriate routes, and endpoints would include assessment of calcium signaling and physiological responses.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for Caloxin 2A1 TFA are not detailed in available sources. The compound has a molecular weight of 1592.54. It is a 15-amino acid peptide (VSNSNWPSFPSSGGG-NH₂) and is supplied as a TFA salt.
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| Toxicity/Toxicokinetics |
Toxicological data for Caloxin 2A1 TFA are not provided in available sources. As a research peptide, its safety profile has not been extensively characterized. It is intended for research use only and not for human consumption.
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| References | |
| Additional Infomation |
Caloxin 2A1 TFA is a novel PMCA inhibitor that inhibits human red blood cell Ca²⁺-Mg²⁺-ATPase. It does not affect basal Mg²⁺-ATPase or Na⁺-K⁺-ATPase. It is supplied for research purposes only. No clinical trial or regulatory approval information is available.
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| Molecular Formula |
C66H92F3N19O24
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|---|---|
| Molecular Weight |
1592.54
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| Exact Mass |
1591.651
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| Related CAS # |
Caloxin 2A1;350670-85-8
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| PubChem CID |
145707883
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
23
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| Rotatable Bond Count |
41
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| Heavy Atom Count |
112
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| Complexity |
3210
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| Defined Atom Stereocenter Count |
12
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| SMILES |
CC(C)[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N5CCC[C@H]5C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)NCC(=O)N)N.C(=O)(C(F)(F)F)O
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| InChi Key |
WWVYZHSQQMQNOR-HPUWVREWSA-N
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| InChi Code |
InChI=1S/C64H91N19O22.C2HF3O2/c1-31(2)52(68)62(103)81-44(30-88)57(98)74-37(21-48(66)90)55(96)78-41(27-85)56(97)73-36(20-47(65)89)54(95)76-39(19-33-22-69-35-13-7-6-12-34(33)35)64(105)83-17-9-15-46(83)61(102)79-42(28-86)58(99)75-38(18-32-10-4-3-5-11-32)63(104)82-16-8-14-45(82)60(101)80-43(29-87)59(100)77-40(26-84)53(94)72-25-51(93)71-24-50(92)70-23-49(67)91;3-2(4,5)1(6)7/h3-7,10-13,22,31,36-46,52,69,84-88H,8-9,14-21,23-30,68H2,1-2H3,(H2,65,89)(H2,66,90)(H2,67,91)(H,70,92)(H,71,93)(H,72,94)(H,73,97)(H,74,98)(H,75,99)(H,76,95)(H,77,100)(H,78,96)(H,79,102)(H,80,101)(H,81,103);(H,6,7)/t36-,37-,38-,39-,40-,41-,42-,43-,44-,45-,46-,52-;/m0./s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-N-[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[2-[(2-amino-2-oxoethyl)amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]butanediamide;2,2,2-trifluoroacetic acid
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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 :~100 mg/mL (~62.79 mM)
DMSO :~100 mg/mL (~62.79 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.57 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 (1.57 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 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 (1.57 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 | 0.6279 mL | 3.1396 mL | 6.2793 mL | |
| 5 mM | 0.1256 mL | 0.6279 mL | 1.2559 mL | |
| 10 mM | 0.0628 mL | 0.3140 mL | 0.6279 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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