计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC 50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi , and cathepsins B and L . K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC 50 values of 0.68 nM and 0.87 nM, respectively
In Vitro
K777 (K11777) can inhibit entry driven by other viral envelope proteins, including 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). K777 inhibits SARS-CoV, HCoV-229E, NL63, MERS-CoV, EBOV, SUDV, TAFV, RESTV, BEBOV, MARV and Nipah pseudovirus entry with IC 50 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. 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 (IC 50 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 Ca 2+ mobilization by itself. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 IFN-γR-KO mice (6-8 weeks of age) injected with Cryptosporidium parvumDosage: 35 mg/kg, 70 mg/kg, and 105 mg/kg Administration: Oral administration; twice a day; for 10 days Result: Rescued mice from otherwise lethal infections.
IC50& Target:CCR4 CYP3
规格
规格或纯度
10mM in DMSO
英文名称
K777
生化机理
K777 是一种强效、口服活性和不可逆的半胱氨酸蛋白酶抑制剂。K777 还是一种强效的 CYP3A4 抑制剂（IC 50 为 60 nM），也是一种选择性 CCR4 拮抗剂，具有强效的趋化抑制作用。K777 还能不可逆地抑制 Cruzain，Cruzain 是一种抗肿瘤药物。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1CCN(CC1)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCC3=CC=CC=C3)/C=C/S(=O)(=O)C4=CC=CC=C4
关联CAS
PubChem CID
MeSH Entry Terms
4-methyl-N-((S)-1-oxo-3-phenyl-1-(((S)-1-phenyl-5- (phenylsulfonyl)pentan-3-yl)amino)propan-2-yl)piperazine-1-carboxamide;4-methylpiperazine-1-carboxylic acid(1-((3-benzenesufonyl-1-phenethylallyl)carbamoyl)-2-phenylethyl)amide;APC 3316;APC-3316;APC3316;C
分子量
574.73
技术文档
高级数据
关联靶点（人）
CTSL
Tclin
组织蛋白酶L1(Cathepsin L1)
(3 活性数据)
CTSS
Tchem
组织蛋白酶S(Cathepsin S)
(1 活性数据)
CTSB
Tchem
组织蛋白酶B(Cathepsin B)
(3 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 233277-99-1，分子式为 C32H38N4O4S，分子量为 574.73 g/mol。
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