GSK2982772
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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
GSK2982772 3D分子结构
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GSK2982772 纯度/质量文件 产品仅供科研
货号：A363017
标准纯度：
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产品说明书
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GSK2982772 质控信息
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] [1]
Administration
p.o., i.v.
Pharmacokinetics
Animal
Rats[1]
Monkeys[1]
Dose
1.1 mg/kg (i.v.)
1.2 mg/kg (i.v.)
Administration
i.v.
i.v.
F
110 ± 20% (p.o.)
86 ± 6% (p.o.)
T1/2
3.9 ± 0.7 h (i.v.)
6.5 ± 1.0 h (i.v.)
Tmax
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.)
Cmax
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
摩尔计算器
总药量计算器
工作液计算器
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
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