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[2-AMINOBENZOYL-GLY1]-GALANIN FRAGMENT (1-10)-LYS(RETRO-M-NITRO-TYR) AMIDE,HUMAN TRIFLUOROACETATE SALT

用途

OM99-2,一种八残基拟肽,人脑膜肽2的紧密结合抑制剂,Ki值为9.58 nM[1]。OM99-2大大促进了BACE1抑制剂的开发[2],具有研究阿尔茨海默病的潜力[3]。

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名称

[ CAS 号 ]:
314266-76-7

[ 中文名 ]:
[2-AMINOBENZOYL-GLY1]-GALANIN FRAGMENT (1-10)-LYS(RETRO-M-NITRO-TYR) AMIDE,HUMAN TRIFLUOROACETATE SALT

[ 英文名 ]:
OM99-2 trifluoroacetate salt

[英文别名 ]:

om99-2
MFCD03787969
H-Glu-Val-Asn-[(2R,4S,5S)-5-amino-4-hydroxy-2

生物活性

[ 描述 ]:

OM99-2,一种八残基拟肽,人脑膜肽2的紧密结合抑制剂,Ki值为9.58 nM[1]。OM99-2大大促进了BACE1抑制剂的开发[2],具有研究阿尔茨海默病的潜力[3]。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> β-分泌

研究领域 >> 神经疾病

[ 靶点 ]

Ki: 9.58 nM (memapsin 2)

[体外研究]

Memapsin 2(BACE)是一种天冬氨酸蛋白酶,称为β-分泌酶,作用于人脑中β-淀粉样肽的产生[4]。

[参考文献]

[1]. Ghosh AK, et al. Design of Potent Inhibitors for Human Brain Memapsin 2 (β-Secretase). J Am Chem Soc. 2000;122(14):3522-3523.

[2]. Zhao J, et al. Targeting Amyloidogenic Processing of APP in Alzheimer's Disease. Front Mol Neurosci. 2020;13:137. Published 2020 Aug 4.

[3]. Dash C, et al. Aspartic peptidase inhibitors: implications in drug development. Crit Rev Biochem Mol Biol. 2003;38(2):89-119.

[4]. Park H, et al. Determination of the active site protonation state of beta-secretase from molecular dynamics simulation and docking experiment: implications for structure-based inhibitor design. J Am Chem Soc. 2003;125(52):16416-16422.

物理化学性质

[ 密度 ]:
1.311g/cm3

[ 沸点 ]:
1322.4ºC at 760mmHg

[ 分子式 ]:
C₄₁H₆₄N₈O₁₄

[ 分子量 ]:
892.99200

[ 闪点 ]:
753.6ºC

[ 精确质量 ]:
892.45400

[ PSA ]:
375.84000

[ LogP ]:
2.00990

[ 折射率 ]:
1.562

[ 储存条件 ]:
-20°C，干燥，密封

MSDS

详细MSDS(安全技术说明书)

安全信息

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

[ 危害码 (欧洲) ]:
Xi

[ 安全声明 (欧洲) ]:
S22-S24/25

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

文献

Inhibitors of Alzheimer's BACE-1 with 3,5-bis-N-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridine structure.

Arch. Pharm. Res. 38(4) , 456-69, (2015)

β-site amyloid precursor protein cleaving enzyme (BACE-1) is a validated target for Alzheimer therapy due to its distinctive role in pathogenesis of AD. In the present contribution, a series of new 3,...

Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor.

Science 290 , 150, (2000)

Memapsin 2 (beta-secretase) is a membrane-associated aspartic protease involved in the production of beta-amyloid peptide in Alzheimer's disease and is a major target for drug design. We determined th...

Chlamydia trachomatis prevalence and chlamydial/HPV co-infection among HPV-unvaccinated young Italian females with normal cytology.

Hum. Vaccin. Immunother. 11(1) , 270-6, (2015)

Infections caused by Chlamydia trachomatis (Ct) and human papillomavirus (HPV) are the two main sexually transmitted infections; however, epidemiological data on Ct prevalence and Ct/HPV co-infection ...

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