胃蛋白酶抑制剂

胃蛋白酶抑制剂用途

Pepstatin 是由放线菌类产生的一种特异性的天冬氨酸蛋白酶 (aspartic proteases) 抑制剂,能够抑制 hemoglobin-pepsin,hemoglobin-proctase,casein-pepsin,casein-proctase,casein-acid protease 和 hemoglobin-acid protease 的活性,IC50 值分别为 4.5 nM,6.2 nM,150 nM,290 nM,520 nM 和 260 nM；同时可抑制 HIV protease 的活性。

胃蛋白酶抑制剂名称

[ CAS 号 ]:
26305-03-3

[ 中文名 ]:
胃酶抑素 A

[ 英文名 ]:
Pepstatin

[中文别名 ]:

[英文别名 ]:

Pepstatin A
Pepstatin (USAN)
pepsininhibitors735a
IHN
peptistatin A
EINECS 247-600-0
Procidin S 735A
procidins735a
PEPSTATIN
ahpatininc

胃蛋白酶抑制剂生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> HIV蛋白酶

信号通路 >> 代谢酶/蛋白酶 >> 蛋白酶体

研究领域 >> 感染

天然产物 >> 其他

多肽产品

[ 靶点 ]

IC50: 4.5 nM (Hemoglobin-pepsin), 6.2 nM (Hemoglobin-proctase), 150 nM (Casein-pepsin), 260 nM (Hemoglobin-acid protease), 290 nM (Casein-proctase), 520 nM (Casein-acid protease)[1]

[体外研究]

Pepstatin是一种由放线菌产生的特异性酸性蛋白酶抑制剂,血红蛋白-胃蛋白酶,血红蛋白-直链酶,酪蛋白-胃蛋白酶,酪蛋白-酪蛋白酶,酪蛋白-的IC50分别为4.5 nM,6.2 nM,150 nM,290 nM,520 nM和260 nM酸性蛋白酶和血红蛋白酸性蛋白酶分别[1]。胃蛋白酶抑制素(Pepstatin A)抑制重组HIV蛋白酶,IC50为250μM。 Pepstatin对细胞蛋白质合成没有影响,可能不会发挥严重的细胞毒性[2]。

[体内研究]

胃蛋白酶抑制剂具有非常低的毒性,通过ip途径对小鼠,大鼠,兔和狗的LD50为1090mg/kg,875mg/kg,820mg/kg和450mg/kg,并且对所有人均为> 2000mg/kg。物种通过口服途径。胃蛋白酶抑制剂(0.5-50 mg/kg,po)抑制结扎Shay大鼠的幽门胃溃疡[1]。

[细胞实验]

胃蛋白酶抑制剂A以7mM新鲜溶解于DMSO中。将其非常缓慢地（1：100）稀释到HIV感染的H9悬浮培养基的培养基中，使得没有胃蛋白酶抑制剂A沉淀（最终浓度，70μM胃蛋白酶抑制剂A和1％DMSO），并且培养物在不改变培养基的情况下孵育。持续48小时。作为对照，未感染的H9细胞也与胃酶抑素一起孵育，此外HIV感染和未感染的细胞与1％DMSO孵育但不含胃蛋白酶抑制剂[2]。

[参考文献]

[1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62.

[2]. Seelmeier S, et al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6.

[相关活性小分子]

胃蛋白酶抑制剂物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
997.6±65.0 °C at 760 mmHg

[ 熔点 ]:
233 °C (dec.)(lit.)

[ 分子式 ]:
C₃₄H₆₃N₅O₉

[ 分子量 ]:
685.892

[ 闪点 ]:
557.1±34.3 °C

[ 精确质量 ]:
685.462585

[ PSA ]:
223.26000

[ LogP ]:
2.16

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.504

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Stable. Incompatible with strong bases, strong acids.

[ 水溶解性 ]:
10% acetic acid in methanol: 1 mg/mL

胃蛋白酶抑制剂MSDS

详细MSDS(安全技术说明书)

胃蛋白酶抑制剂毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SC6155000

CHEMICAL NAME :: Pepstatin A

CAS REGISTRY NUMBER :: 26305-03-3

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C34-H63-N5-O9

MOLECULAR WEIGHT :: 686.02

WISWESSER LINE NOTATION :: QV1YQY1Y1&1&MVY1&MV1YQY1Y1&1&MVYY1&1&MVYY1&1&MV1Y1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PPTCBY Proceedings of the International Symposium of the Princess Takamatsu Cancer Research Fund. (Japan Scientific Soc. Press, 6-2-10 Hongo, Bunkyo-ku, Tokyo 113, Japan) 1st- 1971- Volume(issue)/page/year: 6,57,1976

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 875 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 23,259,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PPTCBY Proceedings of the International Symposium of the Princess Takamatsu Cancer Research Fund. (Japan Scientific Soc. Press, 6-2-10 Hongo, Bunkyo-ku, Tokyo 113, Japan) 1st- 1971- Volume(issue)/page/year: 6,57,1976

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1090 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 23,259,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 23,259,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 450 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 23,259,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 23,259,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 820 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 23,259,1970

胃蛋白酶抑制剂安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ RTECS号 ]:
SC6155000

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