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MK-1064

Name: MK-1064
Brand: TargetMol
SKU: T3722
Price: 569 CNY
Availability: InStock
Rating: 5 (10 reviews)

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纯度: 99.82%

货号 T3722Cas号 1207253-08-4

别名 Urokinase inhibitor 1, MK 1064

MK-1064 (Urokinase inhibitor 1) 是一种选择性食欲素 2 (2-SORA)受体拮抗剂，可用于失眠患者的研究。

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MK-1064

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很棒

纯度: 99.82%

货号 T3722 别名 Urokinase inhibitor 1, MK 1064Cas号 1207253-08-4

MK-1064 (Urokinase inhibitor 1) 是一种选择性食欲素 2 (2-SORA)受体拮抗剂，可用于失眠患者的研究。

规格	价格	库存
1 mg	¥ 569	现货
5 mg	¥ 1,380	现货
10 mg	¥ 2,250	现货
25 mg	¥ 3,850	现货
50 mg	¥ 5,470	现货
100 mg	¥ 7,480	现货
1 mL x 10 mM (in DMSO)	¥ 1,430	现货

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COA HNMR LCMS 产品操作手册

产品介绍

MK-1064 AI Summary

MK-1064 exhibits a diverse range of bioactivities. It demonstrates high binding affinity to the human orexin-2 receptor (OX2R) with a Ki value of 0.5 nM and shows lower affinity for the orexin-1 receptor (OX1R) with a Ki of 1584.0 nM, indicating a selectivity for the orexin-2 receptor. The compound also inhibits the CYP3A4 enzyme with a Ki value of 9500.0 nM and has a Kinact/Ki ratio of 0.012 /min/µM, suggesting slow inactivation relative to its binding affinity, with a Kinact value of 0.11 /min. In terms of bioactivity, MK-1064 shows inhibitory activity against SARS-CoV-2 3CL-Pro protease with 15.3% inhibition at 20 µM and exhibits slight inhibition of virus-induced cytotoxicity in VERO-6 cells. It also participates in modulating cell viability in assays with HEK293T, U2OS, and human fibroblast cells, exhibiting inconsistent effects on cell growth rates. Furthermore, the compound acts as a substrate for human P-glycoprotein with an efflux ratio of 2.4. Pharmacokinetically, the compound has shown effects on sleep parameters in animal models and possesses clearance rates, half-lives, and oral bioavailability. Its thermal stability impacts a range of protein interactions as observed in thermal shift assays, indicating its broad interactive potential. In GPCR beta-arrestin recruitment assays, it shows varying degrees of inhibition and stimulation across multiple targets, highlighting its multifaceted bioactivity profile..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	MK-1064 (Urokinase inhibitor 1) is a selective orexin 2 receptor antagonist (2-SORA).
靶点活性	OX2 receptor:18 nM, OX2 receptor:0.5 nM (Ki), OX1 receptor:1789 nM, OX1 receptor:1584 nM (Ki)
别名	Urokinase inhibitor 1, MK 1064

化学信息

分子量	461.9
分子式	C₂₄H₂₀ClN₅O₃
CAS No.	1207253-08-4
Smiles	COc1ccc(CNC(=O)c2cc(cnc2-c2ccccn2)-c2cncc(Cl)c2)nc1OC
密度	1.305 g/cm3 (Predicted)
颜色	White
物理性状	Solid

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

H2O: < 0.1 mg/mL (insoluble)

DMSO: 50 mg/mL (108.25 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.33 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	2.1650 mL	10.8249 mL	21.6497 mL	108.2485 mL
5 mM	0.4330 mL	2.1650 mL	4.3299 mL	21.6497 mL
10 mM	0.2165 mL	1.0825 mL	2.1650 mL	10.8249 mL
20 mM	0.1082 mL	0.5412 mL	1.0825 mL	5.4124 mL
50 mM	0.0433 mL	0.2165 mL	0.4330 mL	2.1650 mL
100 mM	0.0216 mL	0.1082 mL	0.2165 mL	1.0825 mL