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(2S)-2-[(4S)-2-氨基-1,4,5,6-四羟基4-嘧啶基]-N-[[[(1S)-1-羰基-3-甲基丁基]氨基]羰基]甘氨酰-N1-[(1S)-1-甲基-2-氧乙基-L-谷氨酸甲酰胺

用途

弹性蛋白酶抑制剂是一种有效的竞争性弹性蛋白酶抑制剂,Ki为0.21μM。与白细胞弹性蛋白酶相比,弹性蛋白酶更有效地抑制胰腺弹性蛋白酶。Elastatinal对人白细胞糜蛋白酶样蛋白酶[1][2][3][4]无活性。

名称

[ CAS 号 ]:
51798-45-9

[ 中文名 ]:
(2S)-2-[(4S)-2-氨基-1,4,5,6-四羟基4-嘧啶基]-N-[[[(1S)-1-羰基-3-甲基丁基]氨基]羰基]甘氨酰-N1-[(1S)-1-甲基-2-氧乙基-L-谷氨酸甲酰胺

[ 英文名 ]:
Elastatinal

[英文别名 ]:

elastatinal from microbial source
Leu-co-cpd-Gln-Ala-h
Elastatinal
EINECS 257-426-7

生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 弹性蛋白酶

研究领域 >> 炎症/免疫

[体外研究]

弹性蛋白酶抑制乙酰丙氨酸基丙氨酸对硝基苯胺和乙酰丙氨酸基丙氨酸甲酯与弹性蛋白酶的结合,Kis分别为0.24μM和0.21μM[1]。弹力素(5-20μM)抑制中性粒细胞增强的破骨细胞分化[3]。

[参考文献]

[1]. Umezawa H. Structures and activities of protease inhibitors of microbial origin. Methods Enzymol. 1976;45:678-95.

[2]. Feinstein G, et, al. The inhibition of human leucocyte elastase and chymotrypsin-like protease by elastatinal and chymostatin. Biochim Biophys Acta. 1976 May 13;429(3):925-32.

[3]. Sugisaki R, et, al. Possible involvement of elastase in enhanced osteoclast differentiation by neutrophils through degradation of osteoprotegerin. Bone. 2020 Mar;132:115216.

[4]. Vidhya R, et, al. Anti-inflammatory effects of troxerutin are mediated through elastase inhibition. Immunopharmacol Immunotoxicol. 2020 Oct;42(5):423-435.

物理化学性质

[ 密度 ]:
1.44 g/cm3

[ 分子式 ]:
C₂₁H₃₆N₈O₇

[ 分子量 ]:
512.56

[ 精确质量 ]:
496.27600

[ PSA ]:
224.47000

[ LogP ]:
0.62920

[ 外观性状 ]:
淡黄色固体

[ 折射率 ]:
1.635

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
H2O: 20 mg/mL, clear, yellow

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: LZ9600000

CHEMICAL NAME :: L-Glutamamide, L-2-(2-amino-1,4,5,6-tetrahydro-4-pyrimidinyl-N-(((1- carboxy-3-methylbutyl) amino)carbonyl)glycyl-N(sup 1)-(1-methyl-2-oxoethyl)-, stereoisomer

CAS REGISTRY NUMBER :: 51798-45-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C21-H36-N8-O7

MOLECULAR WEIGHT :: 512.65

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >250 mg/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

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) ]:
22-24/25

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

[ WGK德国 ]:
3

[ RTECS号 ]:
LZ9600000

制备

文献

Elastatinal and leupeptin: effects on u.v.-induced mutation and sister-chromatid exchanges in Chinese hamster cells.

Carcinogenesis 2(4) , 255-9, (1981)

Microbial protease inhibitors elastatinal and leupeptin were tested for cytotoxicity and for effects on spontaneous and u.v.-induced 6-thioguanine-resistant (6TGr) mutation and sister-chromatid exchan...

Reduction of active elastase concentration by means of immobilized inhibitors: a novel therapeutic approach.

Biotechnol. Prog. 20(3) , 968-74, (2004)

The inhibitory power of three different active Nylon membranes, separately loaded with three different protease inhibitors, was studied with the aim of reducing the increased elastase concentration oc...

Effects of inhibitors of membrane signal peptide peptidase on protein translocation into membrane vesicles.

Arch. Microbiol. 153(1) , 90-4, (1989)

The effect of the removal of signal peptides after cleavage of precursor molecules by the signal peptidase I was examined in an in vitro translocation system with Escherichia coli membrane vesicles. T...

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