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Loxistatin Acid(E-64C)

Cat. No. M2823
Loxistatin Acid(E-64C) Structure
Synonym:

NSC 694279, EP 475

Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 270  USD270 In stock
50mg USD 920  USD920 In stock
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Quality Control & Documentation
Biological Activity

Loxistatin Acid (E-64C), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.

Chemical Information
Molecular Weight 314.38
Formula C15H26N2O5
CAS Number 76684-89-4
Form Solid
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Florian Kleemiss, et al. Similarities and Differences between Crystal and Enzyme Environmental Effects on the Electron Density of Drug Molecules

[2] K Fukushima, et al. Identification of glutathione conjugate formed from loxistatin in rats

[3] K Fukushima, et al. An epoxysuccinic acid derivative(loxistatin)-induced hepatic injury in rats and hamsters

[4] K Fukushima, et al. Metabolic fate of loxistatin in rat

[5] H Kondo, et al. Inhibitory effect of oryzacystatins and a truncation mutant on the replication of poliovirus in infected Vero cells

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Keywords: Loxistatin Acid(E-64C), NSC 694279, EP 475 supplier, Cathepsin, inhibitors, activators


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