“angiotensin converting enzyme ace”的搜索结果
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dual TACE/MMPs inhibitor
Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) .
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BACE1 inhibitor
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
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BACE-1 inhibitor
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively.
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BACE1 inhibitor
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
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BACE-1 inhibitor
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
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BACE1 inhibitor
BACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively.
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BACE1 inhibitor
Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
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matrix metalloproteinase-13 (MMP-13) inhibitor
T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes.
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Thrombin inhibitor
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin.
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BACE1 inhibitor
BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer??s disease.
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HCV NS5A inhibitor
Ledipasvir acetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
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MMP inhibitor
Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
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MMP inhibitor
Iincyclinide, also known as CMT-3 and COL-3, is a MMP inhibitor and a chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis.
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TACE/MMP 抑制剂
TMI-1是ADAM17(TACE)和MMP的新型活性双重抑制剂。
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β-secretase/BACE1 抑制剂
Verubecestat (MK-8931)是一种有效的选择性β-分泌酶抑制剂,是BACE1蛋白抑制剂或Beta-site APP裂解酶1抑制剂。
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HIV-1 protease 抑制剂
Nelfinavir是一种有效的口服生物可利用的人类免疫缺陷病毒HIV-1蛋白酶抑制剂(Ki=2 nM ),广泛用于与HIV逆转录酶抑制剂联合治疗HIV感染。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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γ-secretase 抑制剂
Begacestat (GSI-953)是一种新型的选择性淀粉样前体蛋白γ-分泌酶的噻吩磺酰胺抑制剂。
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HIV fusion 抑制剂
Enfuvirtide Acetate (T-20)是一个36个氨基酸的肽段,对应于gp41(HIV-1包膜蛋白的跨膜亚基)区域。
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Selective calpain 抑制剂
Acetyl-Calpastatin (184-210) (human)选择性钙蛋白酶抑制剂。强烈抑制钙蛋白酶I(Ki = 0.2 nM)和II,但不抑制木瓜蛋白酶,胰蛋白酶和组织蛋白酶L(Ki = 6 uM)。增加淀粉样β蛋白(Aβ)42,Aβ40和Aβ42比率的分泌。
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BACE1 抑制剂
Timosaponin B-II是知母草(Liliaceae,根茎)的主要活性成分,对脑缺血性损伤具有保护作用。
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TACE/MMP 抑制剂
TAPI-2是TACE,ADAM,ACE分泌酶和其他MMP(金属蛋白酶)的抑制剂。TAPI-2阻止DCC7,APP,TNFα,L-选择素,NOTCH,TGFα,IL-6R9,erbB2/HER2和ACE的释放。该抑制剂已用于组织培养。
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TACE/MMP 抑制剂
TAPI-0是TACE(IC50 = 50-100 nM)以及其他基质和膜金属蛋白酶的抑制剂。
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BACE1 抑制剂
AMG-8718是一种有效的BACE1抑制剂。
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TACE/MMP 抑制剂
TAPI-1是一种ADAM17/TACE抑制剂, 其对细胞因子受体有抑制作用。
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BACE1 抑制剂
AZD3839是人类BACE1的有效选择性抑制剂,Ki为26.1 nM。
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BACE1 抑制剂
LY2811376是第一种可口服的非肽类BACE1抑制剂,可在动物体内产生显着的Aβ降低作用。
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Gamma-secretase 抑制剂
Semagacestat (LY450139)是一种针对Aβ42,Aβ40和Aβ38的γ-分泌酶阻滞剂,IC50分别为10.9 nM,12.1 nM和12.0 nM。 Semagacestat还抑制Notch信号传导,IC50为14.1 nM。
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- Yesuvadian R, .et al. Potent γ-secretase inhibitors/modulators interact with amyloid-β fibrils but do not inhibit fibrillation: a high-resolution NMR study., Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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Gamma-secretase 抑制剂
BMS-708163 (Avagacestat)是口服生物有效的,选择性的γ-分泌酶抑制剂,作用于Aβ40和Aβ42时,IC50分别为0.3 nM和0.27 nM。
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BACE1 抑制剂
LY2886721是一种有效的,选择性的,口服活性的β位淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 抑制剂。LY2886721是一种新型强效药物,用于治疗阿尔茨海默病的研究。
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- Naomi Ito, .et al. miR-15b mediates oxaliplatin-induced chronic neuropathic pain through BACE1 down-regulation, Br J Pharmacol, 2017, Mar; 174(5): 386-395 PMID: 28012171