购物车

您的购物车当前为空

MRK-560

Name: MRK-560
Brand: TargetMol
SKU: T16133
Price: 248 CNY
Availability: InStock
Rating: 5 (10 reviews)

一键复制产品信息

很棒

纯度: 98.87%

货号 T16133Cas号 677772-84-8

MRK-560 是高效的、口服有效的 γ- 分泌酶抑制剂抑制剂，具有大脑屏障渗透性。

为众多的药物研发团队赋能，

让新药发现更简单！

MRK-560

一键复制产品信息

很棒

纯度: 98.87%

货号 T16133Cas号 677772-84-8

MRK-560 是高效的、口服有效的 γ- 分泌酶抑制剂抑制剂，具有大脑屏障渗透性。

规格	价格	库存
1 mg	¥ 248	现货
5 mg	¥ 579	现货
10 mg	¥ 892	现货
25 mg	¥ 1,490	现货
50 mg	¥ 2,980	现货
100 mg	¥ 4,790	现货
1 mL x 10 mM (in DMSO)	¥ 658	现货

库存状态实时更新，以官网显示为准，现货产品可直接加购物车下单

大包装 & 定制

加入购物车

TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

常见问题解答

选择批次:

纯度: 98.87%

颜色: 白色

性状: Solid

联系我们获取更多批次信息

资源下载:

COA LCMS HNMR 产品操作手册

产品介绍

MRK-560 AI Summary

MRK-560 demonstrates significant bioactivity across various biological assays. Notably, it exhibits potent inhibition of gamma-secretase, reducing amyloid beta levels in multiple cell types including SHSY5Y neuroblastoma cells (IC50 = 0.65 nM), HEK293 cells (IC50 = 65.0 nM), and in HEK293 cells with specific IC50 values of 14.3 nM and 15.0 nM for amyloid beta 40 and 42, respectively. In vivo, the compound effectively lowers brain Abeta(40) levels in APP-YAC transgenic mice with a median effective dose (MED) of 1.0 mg/kg, and reduces Abeta42 production in an APP-Swedish transgenic mouse model at 10 mg/kg. Pharmacokinetically, MRK-560 demonstrates good oral bioavailability with an AUC of 1216.1 ng.hr.mL-1 in Sprague-Dawley rats at a 10 mg/kg dose, and reduces plasma amyloid beta levels by 71.0% in these rats after 3 hours. The compound also shows antiviral properties, inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells at a 10 µM concentration with inhibition rates of 11.23% and 0.51%, respectively, and exhibits 3.759% inhibition of SARS-CoV-2 3CL-Pro protease at 20 µM. Moreover, MRK-560 interacts with multiple proteins, affecting their stability in Thermal Shift Assays and demonstrating a strong bioactive profile in phenotypic assays. It also shows selectivity in its enzymatic inhibition profile, with moderate activity against CYP3A4 and negligible or very weak inhibition against CYP2D6 and CYP2C9..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.

化学信息

分子量	517.92
分子式	C₁₉H₁₇ClF₅NO₄S₂
CAS No.	677772-84-8
Smiles	Fc1ccc(F)c(c1)[C@]1(CC[C@@H](CC1)NS(=O)(=O)C(F)(F)F)S(=O)(=O)c1ccc(Cl)cc1
密度	1.57 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 60 mg/mL (115.85 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.86 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9308 mL	9.6540 mL	19.3080 mL	96.5400 mL
5 mM	0.3862 mL	1.9308 mL	3.8616 mL	19.3080 mL
10 mM	0.1931 mL	0.9654 mL	1.9308 mL	9.6540 mL
20 mM	0.0965 mL	0.4827 mL	0.9654 mL	4.8270 mL
50 mM	0.0386 mL	0.1931 mL	0.3862 mL	1.9308 mL
100 mM	0.0193 mL	0.0965 mL	0.1931 mL	0.9654 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。