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AMG-3969

Chemical Structure : AMG-3969

CAS No.: 1361224-53-4

AMG-3969 (AMG3969, AMG 3969)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 522.4639
Formula C21H20F6N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzenemethanol, 4-[(2S)-4-[(6-amino-3-pyridinyl)sulfonyl]-2-(1-propyn-1-yl)-1-piperazinyl]-α,α-bis(trifluoromethyl)-

References

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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