Grazoprevir potassium salt MK-5172 potassium salt|cas:1206524-86-8|西域试剂

Grazoprevir potassium salt MK-5172 potassium salt,99.40%

产品编号：Bellancom-15298A| CAS NO：1206524-86-8| 分子式：C₃₈H₄₉KN₆O₉S| 分子量：804.99

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15298A	￥800.00	杭州北京（现货）
Bellancom-15298A	￥1500.00	杭州北京（现货）
Bellancom-15298A	￥3000.00	杭州北京（现货）
Bellancom-15298A	￥5000.00	杭州北京（现货）
Bellancom-15298A	￥15000.00	杭州北京（现货）

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Grazoprevir potassium salt MK-5172 potassium salt

产品介绍

Grazoprevir potassium salt (MK-5172 potassium salt) 是选择性的丙型肝炎病毒 NS3/4a蛋白酶抑制剂，作用于 gt1b，gt1a，gt2a，gt2b 和 gt3a的 K_i 分别为 0.01 nM，0.01 nM，0.08 nM，0.15 nM 和 0.90 nM。Grazoprevir potassium salt 抑制 SARS-CoV-2 3CL^pro 活性。

生物活性

Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir potassium salt inhibits SARS-CoV-2 3CL^pro activity.

体外研究

In biochemical assays, Grazoprevir (MK-5172) is effective against a panel of major genotypes and variants engineered with common resistant mutations, with K_i of 0.01±<0.01 nM (gt1b), 0.01±0.01 nM (gt1a), 0.08±0.02 nM (gt2a), 0.15±0.06 nM (gt2b), 0.90±0.2 nM (gt3a), 0.07±0.01 nM (gt1b^R155K), 0.14±0.03 nM (gt1b^D168V), 0.30±0.04 nM (gt1b^D168Y), 5.3±0.9 nM (gt1b^A156T), and 12±2 nM (gt1b^A156V), respectively. In the replicon assay, Grazoprevir demonstrates subnanomolar to low-nanomolar EC₅₀s against genotypes 1a, 1b, and 2a, with EC₅₀s of 0.5±0.1 nM, 2±1 nM, and 2±1 nM for gt1b^con1, gt1a, and gt2a, respectively. Grazoprevir is potent against a panel of HCV replication mutants NS5A (Y93H) (EC₅₀=0.7±0.3 nM), NS5B nucleosides (S282T) (EC₅₀=0.3±0.1 nM), and NS5B (C316Y) (EC₅₀=0.4±0.2). Grazoprevir (MK-5172) maintains the excellent potency against the gt 3a enzyme as well as a broad panel of mutant enzymes, has excellent potency in the replicon system [gt1b IC₅₀(50% NHS)=7.4 nM; gt1a IC₅₀(40% NHS)=7 nM], and shows excellent rat liver exposure.

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

体内研究

Grazoprevir (MK-5172) demonstrates efficacy in vivo against chronic-HCV-infected chimpanzees. When dosed to dogs, Grazoprevir (MK-5172) shows low clearance of 5 mL/min/kg and a 3 h half-life after iv dosing and has good plasma exposure (AUC=0.4 μM h) after a 1 mg/kg oral dose. Dog liver biopsy studies showed that the liver concentration of Grazoprevir after the 1 mg/kg oral dose is 1.4 μM at the 24 h time point. Similar to its behavior in rats, Grazoprevir demonstrates effective partitioning into liver tissue and maintains high liver concentration, relative to potency, 24 h after oral dosing in dogs.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (124.23 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2423 mL	6.2113 mL	12.4225 mL
5 mM	0.2485 mL	1.2423 mL	2.4845 mL
10 mM	0.1242 mL	0.6211 mL	1.2423 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 (sealed storage, away from moisture)。-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 (3.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.11 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% corn oil
Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.11 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。