Chemical Structure : AMG-3969
CAS No.: 1361224-53-4
货号: PC-43024Not For Human Use, Lab Use Only.
AMG-3969 is a potent, metabolically stable Glucokinase (GK)-GKRP (GK regulatory protein) disruptor with IC50 of 4 nM, does not block the GK binding site directly.
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AMG-3969 is a potent, metabolically stable Glucokinase (GK)-GKRP (GK regulatory protein) disruptor with IC50 of 4 nM, does not block the GK binding site directly.
AMG-3969 exhibits robust glucose lowering in diabetic mouse models.
AMG-3969 is highly effective in promoting carbohydrate substrate use, demonstrates a robust pharmacodynamic response (GK translocation, mGKGK translocation EC50=0.2 uM) as well as statistically significant dose-dependent reductions in fed blood glucose levels.
分子量 | 522.4639 | |
分子式 | C21H20F6N4O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Benzenemethanol, 4-[(2S)-4-[(6-amino-3-pyridinyl)sulfonyl]-2-(1-propyn-1-yl)-1-piperazinyl]-α,α-bis(trifluoromethyl)- |
1. Lloyd DJ, et al. Nature. 2013 Dec 19;504(7480):437-40.
2. St Jean DJ Jr, et al. J Med Chem. 2014 Jan 23;57(2):325-38.
3. Nishimura N, et al. J Med Chem. 2014 Apr 10;57(7):3094-116.
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