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134448-10-5

中文名稱 L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE
英文名稱 CA-074
CAS 134448-10-5
分子式 C18H29N3O6
分子量 383.44
MOL 文件 134448-10-5.mol
更新日期 2024/12/03 15:40:35
134448-10-5 結(jié)構(gòu)式 134448-10-5 結(jié)構(gòu)式

基本信息

中文別名
CATHEPSIN B抑制劑(CA-074)
(L-3-反式-(丙基氨基甲酰基)環(huán)氧乙烷-2-羰基)-L-異亮氨酰-L-脯氨酸
英文別名
CA-074
CA-074 >=99% (TLC)
CATHEPSIN B INHIBITOR III
INHIBITOR FOR CATHEPSIN B
L-trans-Epoxysuccinyl(propylamide)-Ile-Pro
L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE
L-TRANS-EPOXYSUCCINYL (PROPYLAMIDE)-ILE-PRO-OH
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-(PROPYLCARBOMOYL)OXIRANE-2-CARBONYL]-L-ISOLEUCYL-L-PROLINE

物理化學性質(zhì)

沸點728.9±60.0 °C(Predicted)
密度1.267±0.06 g/cm3(Predicted)
儲存條件-20°C
溶解度溶于甲醇,濃度為 1mg/ml。也溶于DMSO或乙醇。
酸度系數(shù)(pKa)3.43±0.20(Predicted)
形態(tài)solid
顏色White to yellow

安全數(shù)據(jù)

WGK Germany3
WGK Germany3
L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-103350L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE
CA-074
134448-10-51mg900元
2024/11/08HY-103350L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE
CA-074
134448-10-510mM * 1mLin DMSO2278元
2024/11/08HY-103350L-TRANS-EPOXYSUCCINYL-ILE-PRO-OH PROPYLAMIDE
CA-074
134448-10-55mg2700元

常見問題列表

生物活性
CA-074是組織蛋白酶B (cathepsin B) 的有效抑制劑, Ki 值為2 to 5 nM。
靶點

Ki: 2 to 5 nM (Cathepsin B)

體外研究

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.

體內(nèi)研究

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.

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