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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。
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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 ]:

生物活性

[ 描述 ]:

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。

[ 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

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
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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

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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...


更多文献

推荐生产厂家/供应商:

公司名:上海化源世纪贸易有限公司

区域:上海市普陀区

价格:

联系人:徐乾明

产品详情:(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


公司名:上海脉铂医药科技有限公司

区域:上海市嘉定区

价格:
¥1180.0/5mg ¥2131.0/10mg ¥4284.0/25mg ¥需询单/1g

联系人:李先生

产品详情:Elastatinal


公司名:上海阿拉丁生化科技股份有限公司

区域:上海市浦东新区

价格:
¥1750.9/5mg ¥需询单/1g ¥需询单/1g ¥需询单/1g

联系人:阿拉丁

产品详情:弹性蛋白酶


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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-谷氨酸甲酰胺供应商


热门化合物

CAS号[51798-45-9]化源网提供[(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]MSDS、说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。>>电脑版:(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

标题:51798-45-9_CAS号:51798-45-9_(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 - 化源网 地址:https://m.chemsrc.com/mip/cas/51798-45-9_953415.html