MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

K777

CAS No. : 233277-99-1

MCE 站：K777

产品活性：K777 是一种有效的，口服活性且不可逆的半胱氨酸蛋白酶 (cysteine protease) 抑制剂，也是一种有效的 CYP3A4 抑制剂，IC₅₀ 为 60 nM，是一种选择性的 CCR4 拮抗剂，具有强的趋化性抑制作用。K777 不可逆地抑制锥虫（克鲁斯锥虫的主要半胱氨酸蛋白酶）和组织蛋白酶 B 和 L。K777 是一种广谱抗病毒药物，通过靶向组织蛋白酶介导的细胞进入。K777 抑制 SARS-CoV 和 EBOV 病毒的进入，IC₅₀ 值分别为 0.68 nM 和 0.87 nM。

研究领域：Metabolic Enzyme/Protease  |  Immunology/Inflammation  |  GPCR/G Protein

作用靶点：Cathepsin  |  CCR  |  Cytochrome P450

In Vitro: K777 (K11777) can inhibit entry driven by other viral envelope proteins, HIV-based pseudotypes bearing spikes from coronaviruses (SARS-CoV, HCoV-229E, NL63, MERS-CoV) or glycoproteins from filoviruses (EBOV, SUDV, TAFV, RESTV, BEBOV and MARV) are examined. K777 inhibits SARS-CoV, HCoV-229E, NL63, MERS-CoV, EBOV, SUDV, TAFV, RESTV, BEBOV, MARV and Nipah pseudovirus entry with IC₅₀ values of 0.68 nM, 1.48 nM, 6.78 nM, 46.12 nM, 0.87 nM, 1.14 nM, 2.26 nM, 3.37 nM, 5.91 nM, 1.9 nM and 0.42 nM, respectively. In contrast, 100 nM K777 does not inhibit infection mediated by envelope glycoproteins from an alphavirus (CHIKV), a rhabdovirus (VSV), a flavivirus (HCV), the retroviruses MLV-A and XMRV or two arenaviruses, Lassa and Junin virus.
Whether K777 displays antiviral activity in TMPRSS2 expressing cells are assessed. For this, the incubated target cells with Camostat, K777, or a combination of K777 and Camostat and then infected with pseudoviruses bearing 229E-S. K777 alone demonstrates up to ~ 70% inhibition of 229E-S-mediated transduction. Simultaneous treatment with Camostat and K777 increases inhibition to ~ 90%. Similar inhibition patterns are obtained using the human intestinal epithelial cell line Caco-2, which express endogenous TMPRSS2 and cathepsins.
K777 inhibits both CCL17 binding and CCL17-induced chemotaxis in Hut78 cells (IC₅₀ of 57 and 8.9 nM, respectively). The K777-mediated inhibition of chemotaxis is potent even in the presence of a 10-fold higher concentration of CCL17. K777 induces CCR4 internalization, with a ?50% reduction of cell surface CCR4. K777 does not inhibit CXCR4-induced chemotaxis or internalization and did not bring about Ca²⁺ mobilization by itself.

In Vivo: K777 (K11777; 35-105 mg/kg; oral administration; twice a day; for 10 days; C57BL/6 IFN-γR-KO mice) treatment rescues mice from otherwise lethal infections .

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Antioxidants Compound Library  |  Oxygen Sensing Compound Library  |  Leupeptin hemisulfate  |  Pirfenidone  |  Aloxistatin  |  N-Ethylmaleimide  |  Verapamil hydrochloride  |  PMSF  |  Maraviroc  |  Apigenin  |  E-64  |  Fenofibrate  |  CA-074 methyl ester  |  Ketoconazole  |  1-Aminobenzotriazole  |  Itraconazole  |  RS 504393  |  Abiraterone  |  CA-074  |  Calpeptin  |  INCB3344  |  PF-4136309  |  Papain  |  Bindarit  |  Talarozole  |  Clarithromycin  |  BX471  |  LY 3000328  |  Atazanavir sulfate  |  Isavuconazole  |  Atovaquone

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。