Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Calpeptin (sequence: Z-Leu-nLeu-H) is a novel, potent, cell-permeable calpain inhibitor that has anti-fibrotic properties. With IC50s of 52 nM, 34 nM, 138 nM, and 40 nM, respectively, it inhibits Calpain I (porcine erythrocytes), Calpain II (porcine kidney), and Calpain I (human platelets). In an rat model of multiple sclerosis, it reduces apoptosis, inflammation, cell death, and axonal damage. Calpeptin also inhibited the migration of cells that was dependent on angiopoietin-1 and the proliferation of cells that was dependent on IL-6. This may be the fundamental mechanism underlying Calpeptin's protective effect against pulmonary fibrosis.
Targets |
Calpain II (ID50 = 34 nM); Calpain I (ID50 = 40 nM); Calpain I (ID50 = 52 nM); Papainb (ID50 = 138 nM)
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ln Vitro |
Calpeptin inhibits thrombin, ionomycin, or collagen-stimulated platelets' 20K phosphorylation in a dose-related manner.[1] By inhibiting Calpain activity, capeptin stimulates neurite elongation in PC12 cells that are differentiating.[2] Calpeptin functions as a functional neuroprotectant in rat retinal ganglion cells by reducing apoptosis and preserving the normal whole-cell membrane potential.[3]
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ln Vivo |
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Enzyme Assay |
Calpeptin (0.6 mg/kg, i.v.) inhibits the activation of calpain and caspase-3, cleavage of their substrates, and cardiomyocyte programmed cell death in a feline right ventricular (RV) PO (RVPO) model.[4] Through the inhibition of Caspase-3 expression, Calpeptin lowers the neuronal apoptosis in the hippocampal CA1 sector in a rat focal cerebral ischemia–reperfusion injury model.[5]
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Cell Assay |
Calpeptin inhibited lung fibroblasts' ability to produce TGF-b1, IL-6, angiopoietin-1, and collagen. Calpeptin also inhibited the migration of cells that was dependent on angiopoietin-1 and the proliferation of cells that was dependent on IL-6. This may be the fundamental mechanism underlying Calpeptin's protective effect against pulmonary fibrosis.
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Animal Protocol |
C57BL/6 female mice (Eight-week-old)[3]
0.04 mg/mouse. Intraperitoneally three times weekly for 28 days (together with Bleo). |
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References |
Molecular Formula |
C20H30N2O4
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Molecular Weight |
362.46
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Exact Mass |
362.22
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Elemental Analysis |
C, 66.27; H, 8.34; N, 7.73; O, 17.66
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CAS # |
117591-20-5
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
CCCC[C@@H](C=O)NC(=O)[C@H](CC(C)C)NC(=O)OCC1=CC=CC=C1
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InChi Key |
PGGUOGKHUUUWAF-ROUUACIJSA-N
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InChi Code |
InChI=1S/C20H30N2O4/c1-4-5-11-17(13-23)21-19(24)18(12-15(2)3)22-20(25)26-14-16-9-7-6-8-10-16/h6-10,13,15,17-18H,4-5,11-12,14H2,1-3H3,(H,21,24)(H,22,25)/t17-,18-/m0/s1
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Chemical Name |
benzyl N-[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxohexan-2-yl]amino]pentan-2-yl]carbamate
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Synonyms |
Calpain; N-Cbz-leu-nleu-al; Benzylcarbonyl-leu-nleu-H
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.90 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 (6.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7589 mL | 13.7946 mL | 27.5893 mL | |
5 mM | 0.5518 mL | 2.7589 mL | 5.5179 mL | |
10 mM | 0.2759 mL | 1.3795 mL | 2.7589 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.