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Purity: ≥98%
Loxistatin Acid (formerly also known as E-64C; NSC-694279; EP-475), an analog of E-64, is a novel, potent, irreversible and membrane-permeable cysteine protease inhibitor with important biological activity. Using cathepsins B and L, it has been shown that E-64-c is significantly more reactive than E-64. To measure the rate constants of inhibition of E-64-c, human liver cathepsins B and H and rat cathepsin L were utilized. The results showed that the rate constants of inactivation of cathepsins B, H, and L were, respectively, 298000, 2018, and 206000 M-1 s-1.
| Targets |
Cysteine proteases; CANP; Cathepsin C
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| ln Vitro |
Loxistatin Acid (E-64C) normalizes the increased activities of cathepsin B and cathepsin H in the pectoral muscle of dystrophic chickens.[2] After the middle cerebral artery in rats is blocked, E-64C prevents the ischemic degradation of cerebral proteins.[3]
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| ln Vivo |
Loxistatin Acid (E-64C), as a thiol protease inhibitor, inhibits calpain activity in intact platelets.[1] E-64C shows promise as a treatment for Alzheimer's disease because it reduces the production of Aβ and inhibits β-secretase activity in the regulated secretory vesicles of neuronal chromaffin cells.[4]
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| Animal Protocol |
Dogs: Research is conducted on 83 mongrel dogs weighing an average of 11.2 kg. Through intravenous sodium thiamylal (7 mg/kg), they are rendered unconscious. Group A (n = 17) receives an intravenous bolus of E-64c (100 mg/kg) dissolved in saturated sodium bicarbonate just prior to the occlusion and following reperfusion, while Group B (n = 17) only receives the vehicle solution during these periods. The LAD is permanently ligated at the same level in the 49 dogs that remain (Groups C and D). An intravenous bolus of either vehicle only (Group D; n = 25) or loxstatin acid (100 mg/kg) is administered just prior to and one hour following the ligation. The estimated intramyocardial Loxistatin acid molecular concentration is 1,000 times that of total mCANP, and the dose of E-64c is intended for potential use in clinical practice.
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| References |
| Molecular Formula |
C15H26N2O5
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| Molecular Weight |
314.38
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| Exact Mass |
314.18
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| Elemental Analysis |
C, 57.31; H, 8.34; N, 8.91; O, 25.45
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| CAS # |
76684-89-4
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC(C)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1[C@H](O1)C(=O)O
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| InChi Key |
SCMSYZJDIQPSDI-SRVKXCTJSA-N
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| InChi Code |
InChI=1S/C15H26N2O5/c1-8(2)5-6-16-13(18)10(7-9(3)4)17-14(19)11-12(22-11)15(20)21/h8-12H,5-7H2,1-4H3,(H,16,18)(H,17,19)(H,20,21)/t10-,11-,12-/m0/s1
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| Chemical Name |
(2S,3S)-3-[[(2S)-4-methyl-1-(3-methylbutylamino)-1-oxopentan-2-yl]carbamoyl]oxirane-2-carboxylic acid
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| Synonyms |
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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: ≥ 2.08 mg/mL (6.62 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 20.8 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: ≥ 2.08 mg/mL (6.62 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 20.8 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: ≥ 2.08 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 2mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1809 mL | 15.9043 mL | 31.8086 mL | |
| 5 mM | 0.6362 mL | 3.1809 mL | 6.3617 mL | |
| 10 mM | 0.3181 mL | 1.5904 mL | 3.1809 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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