K777|cas:233277-99-1|西域试剂

K777,99.60%

产品编号：Bellancom-119293| CAS NO：233277-99-1| 分子式：C₃₂H₃₈N₄O₄S| 分子量：574.73

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货号	价格	库存与货期
Bellancom-119293	￥3800.00	杭州北京（现货）
Bellancom-119293	￥6400.00	杭州北京（现货）
Bellancom-119293	￥13200.00	杭州北京（现货）

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K777

产品介绍

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 是一种广谱抗病毒活性分子，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。

生物活性

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC₅₀ 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 IC₅₀ values of 0.68 nM and 0.87 nM, respectively.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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^[4] .

西域 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 parvum^[4]
Dosage:	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.

体内研究

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^[4] .

西域 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 parvum^[4]
Dosage:	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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (173.99 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7399 mL	8.6997 mL	17.3995 mL
5 mM	0.3480 mL	1.7399 mL	3.4799 mL
10 mM	0.1740 mL	0.8700 mL	1.7399 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.35 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。