ml 128

VU0361737 (ML-128) 是一种高效选择性的，中枢神经系统渗透性的代谢型谷氨酸受体 4(mGluR4)正变构调节剂，对人类和大鼠 mGluR4作用的EC50值分别为 240 和 110 nM。它具有神经保护作用，有用于帕金森氏病的研究潜力。

YKAs3003, a potent inhibitor of pathogenic KAS III, displays minimal inhibitory concentration (MIC) values in the range 128-256 microg/mL against various bacteria.

β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but not of resistantM. tuberculosisRM22 when used at a concentration of 128 μg/ml.3,4It blocks human and mouse Kv1.3 voltage-gated potassium channels (IC50s = 11.8 and 13.2 μM, respectively).5Overexpression of β-defensin-1 in the human oral squamous cell carcinoma (OSCC) cell lines HSC-3, UM-1, and SCC-9 increases migration and invasion but not proliferation.6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Schroeder, B.O., Ehmann, D., Precht, J.C., et al.Paneth cell α-defensin 6 (HD-6) is an antimicrobial peptideMucosal Immunol.8(3)661-671(2015) 3.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 4.Fattorini, L., Gennaro, R., Zanetti, M., et al.In vitro activity of protegrin-1 and beta-defensin-1, alone and in combination with isoniazid, against Mycobacterium tuberculosisPeptides25(7)1075-1077(2004) 5.Feng, J., Xie, Z., Yang, W., et al.Human beta-defensin 1, a new animal toxin-like blocker of potassium channelToxicon113(2016) 6.Han, Q., Wang, R., Sun, C., et al.Human beta-defensin-1 suppresses tumor migration and invasion and is an independent predictor for survival of oral squamous cell carcinoma patientsPLoS One9(3)e91867(2014)

Leoidin is a depsidone originally isolated from L. gangaleoides that has antibacterial and enzyme inhibitory activities.1,2,3 It is active against the bacteria E. faecalis, H. influenzae, M. catarrhalis, S. aureus, and S. pneumoniae (MICs = 8, 32, 1, 128, and 64 μg ml, respectively).2 Leoidin inhibits phenylalanyl-tRNA synthetase (PheRS) isolated from P. aeruginosa (IC50 = 42 μM). It also inhibits organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 with Ki values of 0.08 and 1.84 μM, respectively, in CHO cells expressing the human transporters.3

(-)-Mycousnine is a microbial metabolite and derivative of usnic acid originally isolated fromM. nawaethat has antibacterial and antifungal activities.1,2It is active against the Gram-positive bacteriaB. subtilis,K. rhizophila, andS. aureus(MICs = 4, 8, and 4 g ml, respectively) but not the Gram-negative bacteriaE. coli,S. typhimurium, andK. pneumoniae(MICs = >128 g ml for all).2(-)-Mycousnine is also active against the fungiT. mentagrophytes,T. rubrum, andC. albicans(MICs = 25, 25, and 100 μg ml, respectively).1 1.Sassa, T., and Igarashi, M.Structures of (-)-mycousnine, (+)-isomycousnine and (+)-oxymycousnine, new usnic acid derivatives from phytopathogenic Mycosphaerella nawaeAgric. BioI. Chem.54(9)2231-2237(1990) 2.Lee, J., Lee, J., Kim, G.J., et al.Mycousfurans A and B, antibacterial usnic acid congeners from the fungus Mycosphaerella sp., isolated from a marine sedimentMar. Drugs17(7)422(2019)

A-39183A is an active component of the A-39183 antibiotic complex produced by aerobic fermentation of Streptomyces NRRL 12049. It has activity against penicillin-resistant S. aureus 3055 and S. faecalis X66 (MICs = 32 and 32 μg/ml, respectively) and a variety of Gram-positive and Gram-negative anaerobic bacteria (MICs = 16-128 μg/ml) in an agar dilution assay.

Antibacterial agent 50 (example 47) is a compound that exhibits antibacterial activity. It shows minimum inhibitory concentration (MIC) values of 32, 64, and 128 mcg mL against three strains of E. coli, namely NCTC 13351, M 50, and 7 MP, respectively (WO2013030733A1).

Antitubercular agent-17 (Compound 8a) 是一种抗结核剂，对 M. tuberculosisH37Rv、Spec. 192、Spec 210 和 Spec. 800 的 MIC 值分别为 2、2、2 和 128 μg ml。Antitubercular agent-17 表现出高选择性的抗分支杆菌效果。

Antitubercular agent-18 (Compound 9a) 为抗结核剂，对M. tuberculosisH37Rv、Spec. 192、Spec 210 及 Spec. 800 的最小抑制浓度(MIC)值依次为2、2、2 及128 μg ml，展现出对分支杆菌的高选择性抗菌活性。

ATP synthase inhibitor2 是一个铜绿假单胞菌 (PA)ATP synthase 抑制剂 (IC50=10 μg mL)，在 128 μg mL 时可完全抑制铜绿假单胞菌 (PA) 的 ATP 合成活性。

Antimicrobial Agent-1 (compound 6C) shows strong activity (MIC = 2 μg mL) against TolC mutant E. coli. Additionally, it synergistically interacts with Colistin to exhibit enhanced activity against Gram-negative bacteria. Importantly, Antimicrobial Agent-1 exhibits no cytotoxic effects on mammalian cell lines. Its MIC values on Caco-2 and Vero cell lines are greater than 128 μg mL [1].

Antibacterial agent 128 是一种带有可裂解接头的铁载体类似物-环丙沙星 (Ciprofloxacin (Ciprofloxacin )) 偶联物。Antibacterial agent 128 显示出针对铜绿假单胞菌 (MIC 值为 0.25-64 μg mL) 和类鼻疽伯克氏菌 (MIC 值为 1-32 μg mL) 的抗生素活性。

ATP synthase inhibitor2 (Compound 22) TFA 为针对铜绿假单胞菌 (PA) ATP synthase 的抑制剂，具IC50值为10 μg mL，在浓度达到128 μg mL 时能够全面阻断铜绿假单胞菌 (PA) ATP的合成活性。

Ranalexin为一抗菌肽，对金黄色葡萄球菌、大肠杆菌及铜绿假单胞菌的最小抑菌浓度(MIC)分别为4、32、128 μg mL。

Lynronne-3 是一种具有抗革兰氏阳性细菌活性的抗菌肽，涵盖 MDR 菌株（对MRSA菌株的 MIC 为 32-128 μg mL）。此外，Lynronne-3 亦对 P. aeruginosa 感染显示出效力。

GP-2B是一种具有针对革兰氏阳性菌株抗菌活性的抗菌肽，其最小抑菌浓度(MIC)针对金黄色葡萄球菌和粪肠球菌为8-128μg mL。

IMCTA-C14是一种洗涤剂且是微生物代谢产物4-糖腺苷的衍生物。其临界胶束浓度(CMC)为0.11 mM，亲水亲油平衡(HLB)值为9.72。IMCTA-C14（0.05%和0.5%）能从OVK18卵巢癌细胞提取蛋白质，包括膜蛋白。它对几种不同菌株具有活性（MICs = 8-128 µg ml），并对52种癌细胞系具有细胞毒性（IC50s = 2.9-29.2 µg ml）。IMCTA-C14（50 µM）诱导OVK18细胞的自噬。

Antibioticadjuvant 1 (compound 3e) 作为抗生素佐剂,虽其自身的抗菌活性较低 (MIC > 128 µg mL),却能显著提升Cloxacillin的效果,增效倍数达66倍,显示出协同增效作用.

1-(3,4-Dimethoxyphenyl)-2-(4-allly-2,6-dimethoxyphenoxy)propan-1-ol shows anti-staphylococcal activity against a total of five multidrug-resistant (MDR) and methicillin-resistant Staphylococcus aureus strains and the minimum inhibitory concentrations (MIC

Sinapaldehyde (trans-3,5-Dimethoxy-4-hydroxy cinnamaldehyde) 对耐甲氧西林的金黄色葡萄球菌和大肠杆菌有抗菌作用，MIC 值都为 128 μg mL。

Chalepensin 是一种从芸香科植物 Ruta chalepensis L. 分离得到的呋喃香豆素，是一种选择性 CYP2A6 抑制剂，抑制 CYP1A1、CYP1A2、CYP2A13、CYP2C9、CYP2D6、CYP2E1 和 CYP3A4。Chalepensin 具有抗原生动物活性，抑制耐甲氧西林金黄色葡萄球菌 （MRSA），MIC值在32-128 μg mL范围内。