S81535 |
GSK180736A |
源葉(MedMol) | 98% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM
- 靶點: ROCK1:100 nM (IC50);GRK2:770 nM (IC50);ROCK;?GRK;?PKA
- 體外研究:
GSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC50 of 0.77 μM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50=100 nM)
- 參考文獻:
1. Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59(8):3793-807.
- 溶解性: soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.737 ml 13.685 ml 27.37 ml 5 mM 0.547 ml 2.737 ml 5.474 ml 10 mM 0.274 ml 1.369 ml 2.737 ml 50 mM 0.055 ml 0.274 ml 0.547 ml
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質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)