抑肽素 A

抑肽素 A化学性质

熔点 :233 °C (dec.)(lit.)
比旋光度 :D27 -90.3° (c = 0.288 in methanol)
沸点 :695.91°C (rough estimate)
密度 :1.1340 (rough estimate)
折射率 :1.7500 (estimate)
储存条件 :2-8°C
溶解度 :10% acetic acid in methanol: 1 mg/mL
酸度系数(pKa) :4.17±0.10(Predicted)
形态 :White solid
颜色 :Colorless needles
旋光性 (optical activity) :Optical rotation: -90.0 ± 5° (c = 0.5, MeOH, 20°C).
水溶解性 :It is soluble in 10% (v/v) acetic acid in methanol (9:1 methanol:acetic acid) (1 mg/ml), ethanol (1-2 mg/ml with heat up to 60°C), DMSO (5 mg/ml), methanol (1 mg/ml), and acetic acid. Insoluble in benzene, chloroform, water, 1 M NaOH, and ether.
BRN :2201362
稳定性 :Stable. Incompatible with strong bases, strong acids.
InChIKey :JKGWASGTXVCDML-LXTPJMTPSA-N
CAS 数据库 :26305-03-3(CAS DataBase Reference)

安全信息

安全说明 :22-24/25
WGK Germany :2
RTECS号 :SC6155000
F :10
海关编码 :29241990
毒性 :LD50 in mice, rats, rabbits, dogs (mg/kg): 1090, 875, 820, 450 i.p.; all >2000 orally (Umezawa, 1970)

抑肽素 A MSDS

生物活性 Pepstatin A (Pepstatin) 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。Pepstatin A 也是 cathepsins D 和 cathepsins E 的抑制剂。Pepstatin A 通过抑制溶酶体蛋白酶来抑制自噬。
靶点
Target Value
aspartic protease
()
cathepsins D
()
cathepsins E
()
体外研究
Pepstatin A对天冬氨酸蛋白酶比如蛋白质，组织蛋白酶D和E表现出有效的抑制作用。在HIV感染的H9细胞中，pepstatin A抑制部分细胞内HIV gag蛋白质的合成，而对HIV感染的细胞没有显著毒性。 Pepstatin A通过阻断ERK信号并抑制NFATc1的表达抑制破骨细胞的增殖。
体内研究

Pepstatin (Pepstatin A) has a very low toxicity, with LD ₅₀ s of 1090 mg/kg, 875 mg/kg, 820 mg/kg and 450 mg/kg for mice, rats, rabbits, and dogs by i.p. route, and > 2000 mg/kg for all species by oral route. Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats.