L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH

Name	L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE
Synonyms	CA-074 INHIBITOR FOR CATHEPSIN B CATHEPSIN B INHIBITOR III L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH L-trans-Epoxysuccinyl(propylamide)-Ile-Pro L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE CA-074(L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE) N-(L-3-TRANS-PROPYLCARBAMOYL-OXIRANE-2-CARBONYL)-ILE-PRO-OH (L-3-TRANS-(PROPYLCARBAMYL)OXIRANE-2-CARBONYL)-L-ISOLEUCYL-L-PROLINE [L-3-TRANS-(PROPYLCARBAMOYL)OXIRANE-2-CARBONYL]-L-ISOLEUCYL-L-PROLINE N-(L-3-trans-PropylcarbaMoyl-oxirane-2-carbonyl)-Ile-Pro-OH, CA-074, L-trans-Epoxysuccinyl(propylaMide)-Ile-Pro-OH
CAS	134448-10-5
EINECS	200-258-5

Molecular Formula	C18H29N3O6
Molar Mass	383.44
Density	1.267±0.06 g/cm3(Predicted)
Boling Point	728.9±60.0 °C(Predicted)
Solubility	Soluble in methanol at 1mg/ml. Also soluble in DMSO or ethanol.
Appearance	solid
pKa	3.43±0.20(Predicted)
Storage Condition	-20°C
In vitro study	CA-074 is a synthetic analogue of E-64, a natural peptidyl epoxide that irreversibly inhibits most known lysosomal cysteine proteinases, and is developed by means of rational drug design, exploiting the dipeptidylcarboxypeptidase activity of cathepsin B. CA-074 can be used to selectively inhibit cathepsin B within living cells, as long as the experimental conditions permit significant fluid-phase endocytosis of the drug. CA-074 inhibits cathepsin B with a K i of 2 to 5 nM, whereas the initial K i s for cathepsin H and L are about 40-200 μM. CA-074 exhibits 10000-30000 times greater inhibitory effects on purified rat cathepsin B than on cathepsin H and L.
In vivo study	Intraperitoneally injection of compound CA-074 into rats potently and selectively inhibits cathepsin B activity. Intravenously administration of CA-074 immediately after the ischaemic insult saves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 min brain ischaemia: the extent of inhibition is excellent in three of eight and good in five of eight monkeys.

WGK Germany

Last Update：2024-01-02 23:10:35

biological activity	CA-074 is a potent inhibitor of cathepsin B with Ki values of 2 to 5 nM.
Target	Ki: 2 to 5 nM (Cathepsin B)

Last Update：2024-04-09 20:45:29

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Product Name: L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE Visit Supplier Webpage Request for quotation
CAS: 134448-10-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH

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