GSK2982772 | RIPK1 Inhibitor | AmBeed-信号通路专用抑制剂

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GSK2982772 99%+

货号：A363017

GSK2982772 is an inhibitor of receptor interacting protein 1 (RIP1) with IC50 of 16 nM and it is used for the treatment of inflammatory diseases.

GSK2982772 化学结构
CAS号：1622848-92-3

GSK2982772 3D分子结构
CAS号：1622848-92-3

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GSK2982772 纯度/质量文件产品仅供科研

货号：A363017 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

NF-κB 亚型比较

产品名称	NF-κB ↓ ↑	其他靶点	纯度
Pyrrolidinedithiocarbamate ammonium	✔		98%
QNZ	++++ NF-κB, IC50: 11 nM		99%+
Sodium 4-Aminosalicylate Dihydrate	✔		98%
Sodium Salicylate	✔		95%
Parthenolide	✔	p53	97% HPLC
JSH-23	+ NF-κB, IC50: 7.1 μM		98%
Phenethyl caffeate	✔		98%
Andrographolide	✔		98+%
Curcumin	✔	HDAC,Nrf2	98%
SC75741	+++ NF-κB, EC50: 200 nM		99%+
CBL0137 HCl	++ NF-κB, EC50: 0.47 μM	p53	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

GSK2982772 生物活性

靶点	TNF-α human RIP1, IC50:16 nM
描述	GSK2982772 is an optimized RIP1 kinase inhibitor with IC50 value of 1nM in a FP/ADP-Glo assay, which is a clinical candidate currently in phase 2a clinical studies for psoriasis, rheumatoid arthritis, and ulcerative colitis. It inhibited U937 cell viability with IC50 value of 6.3nM. Treatment with GSK2982772 at 300nM overnight reduced IL-1β and IL-6 production by ~60% in human explant samples taken from ulcerative colitis patients. GSK2982772 dosed orally 15 min prior to TNF and showed 68, 80 and 87% protection from temperature loss over 6 h, at doses of 3, 10, and 50 mg/kg, respectively. It showed 13, 63, and 93% protection from temperature loss over 3h in the corresponding TNF/zVAD model^[2].
作用机制	GSK2982772 packed against 2 β-strands defined by Leu90-Val91-Met92 and Ile43-Met44-Lys45 of RIP1 kinase, siting deeper in the ATP binding pocket and occupying an allosteric lipophilic pocket at the back through the benzyl group.^[2]

GSK2982772 动物研究

Dose

Mice: 50 mg/kg^[1] (p.o.); 3 mg/kg - 50 mg/kg^[1] (i.v.)

Administration

p.o., i.v.

Pharmacokinetics

Animal	Rats^[1]	Monkeys^[1]
Dose	1.1 mg/kg (i.v.) 2.1 mg/kg (p.o.)	1.2 mg/kg (i.v.) 1.9 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.
F	110 ± 20% (p.o.)	86 ± 6% (p.o.)
T_1/2	3.9 ± 0.7 h (i.v.)	6.5 ± 1.0 h (i.v.)
T_max	0.25 ± 0.0 h (p.o.)	1.8 ± 1.1 h (p.o.)
CL	17 ± 5 ml/min/kg (i.v.)	10 ± 3 ml/min/kg (i.v.)
C_max	810 ± 160 μg/ml (p.o.)	720 ± 240 μg/ml (p.o.)
Vss	2.7 ± 0.6 L/kg (i.v.)	2.2 ± 0.9 L/kg (i.v.)
AUC	2.3 ± 0.8 μg·h/ml (p.o.)	2.9 ± 0.8 μg·h/ml (p.o.)

GSK2982772 参考文献

[1]Harris PA, Berger SB, et al. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261.

[2]Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Eidam PM, Finger JN, Hoffman SJ, Kang J, Kasparcova V, King BW, Lehr R, Lan Y, Leister LK, Lich JD, MacDonald TT, Miller NA, Ouellette MT, Pao CS, Rahman A, Reilly MA, Rendina AR, Rivera EJ, Schaeffer MC, Sehon CA, Singhaus RR, Sun HH, Swift BA, Totoritis RD, Vossenkämper A, Ward P, Wisnoski DD, Zhang D, Marquis RW, Gough PJ, Bertin J. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261. doi: 10.1021/acs.jmedchem.6b01751. Epub 2017 Feb 10. PMID: 28151659.

GSK2982772 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.65mL

0.53mL

0.26mL

13.25mL

2.65mL

1.32mL

26.50mL

5.30mL

2.65mL

GSK2982772 技术信息

CAS号	1622848-92-3
分子式	C₂₀H₁₉N₅O₃
分子量	377.397

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 250 mg/mL(662.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

GSK2982772 99%+

GSK2982772 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

GSK2982772 质控信息

GSK2982772 生物活性

GSK2982772 动物研究

GSK2982772 参考文献

GSK2982772 实验方案

GSK2982772 技术信息

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GSK2982772 99%+

GSK2982772 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK2982772 质控信息

GSK2982772 生物活性

GSK2982772 动物研究

GSK2982772 参考文献

GSK2982772 实验方案

GSK2982772 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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GSK2982772 纯度/质量文件产品仅供科研