26305-03-3
中文名称
抑肽素
英文名称
Pepstatin
CAS
26305-03-3
EINECS 编号
247-600-0
分子式
C34H63N5O9
MDL 编号
MFCD00060740
分子量
685.89
MOL 文件
26305-03-3.mol
更新日期
2024/04/24 17:01:10
26305-03-3 结构式
基本信息
中文别名
抑肽素胃蛋白酶抑制剂
胃酶抑素
英文别名
(3S,4S)-4-AMINO-3-HYDROXY-6-METHYL-HEPTANOIC ACIDAHMHA ISOVALERYL-L-VAL-L-VAL-AHMHA-L-ALA-STA
ISOVALERYL-L-VAL-L-VAL-AHMHA-L-ALA-AHMHA STA
ISO-VALERYL-L-VAL-L-VAL-STA-L-ALA-STA
ISOVALERYL-L-VAL-L-VAL-STATINYL-L-ALA-STATINE
ISOVALERYL-L-VALYL-L-VALYL-[(3S,4S)-4-AMINO-3-HYDROXY-6-METHYLHEPTANOYL]-L-ALANYL[(3S,4S)-4-AMINO-3-HYDROXY-6-METHYLHEPTANOIC ACID]
ISOVALERYL-L-VALYL-L-VALYL-4-AMINO-3-HYDROXY-6-METHYLHEPTANOYL-L-ALANYL-4-AMINO-3-HYDROXY-6-METHYLHEPTANOIC ACID
ISOVALERYL-VAL-VAL-4-AMINO-3-HYDROXY-6-METHYLHEPTANOYL-ALA-4-AMINO-3-HYDROXY-6-METHYLHEPTANOIC ACID
ISOVALERYL-VAL-VAL-STA-ALA-STA
ISOVALERYL-VAL-VAL-STA-ALA-STA-OH
ISOVALERYL-VAL-VAL-STA-ALA-STA-OH (MICROBIAL PRODUCT)
ISOVAL-VAL-VAL-4-AMINO-3-HYDROXY-5-METHYLHEPTANOYL-ALA-4-AMINO-3-HYDROXY-6-METHYLHEPTANOIC ACID
ISOVAL-VAL-VAL-STA-ALA-STA
I-VALERYL-L-VAL-L-VAL-AHMHA-L-ALA-AHMHA
IVA-VAL-VAL-STA-ALA-STA
PEPSTATIN
PEPSTATIN A
X-VAL-VAL-STATYL-ALA-STATIN
ahpatininc
pepsininhibitors735a
所属类别
生物化工：酶及辅酶类物理化学性质
熔点233 °C (dec.)(lit.)
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
储存条件2-8°C
溶解度10% acetic acid in methanol: 1 mg/mL
溶解度10% 乙酸甲醇溶液：1 mg/mL
酸度系数(pKa)4.17±0.10(Predicted)
形态白色固体
颜色无色针状
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.
BRN2201362
稳定性稳定的。与强碱、强酸不相容。
InChIKeyJKGWASGTXVCDML-LXTPJMTPSA-N
安全数据
警示词警告
危险性描述H315-H319-H335
安全说明22-24/25
安全说明S22-S24/25
WGK Germany2
WGK Germany2
RTECS号SC6155000
F10
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)
常见问题列表
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.