AMG-3969
- Product Name
- AMG-3969
- CAS No.
- 1361224-53-4
- Chemical Name
- AMG-3969
- Synonyms
- CS-2503;AMG-3969;AMG-3969, 10 mM in DMSO;AMG-3969; AMG 3969; AMG3969;Hexokinase IV,AMG 3969,Hexokinase D,Glucokinase,Inhibitor,AMG3969,AMG-3969,inhibit;2-[4-[(2S)-4-[(6-amino-3-pyridyl)sulfonyl]-2-prop-1-ynyl-piperazin-1-yl]phenyl]-1,1,1,3,3,3-hexafluoro-propan-2-ol;Benzenemethanol, 4-[(2S)-4-[(6-amino-3-pyridinyl)sulfonyl]-2-(1-propyn-1-yl)-1-piperazinyl]-α,α-bis(trifluoromethyl)-;(S)-2-(4-(4-((6-Aminopyridin-3-yl)sulfonyl)-2-(prop-1-yn-1-yl)piperazin-1-yl)phenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol
- CBNumber
- CB73166063
- Molecular Formula
- C21H20F6N4O3S
- Formula Weight
- 522.46
- MOL File
- 1361224-53-4.mol
AMG-3969 Property
- Boiling point:
- 648.8±65.0 °C(Predicted)
- Density
- 1.56±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C(protect from light)
- solubility
- DMSO:100.0(Max Conc. mg/mL);191.4(Max Conc. mM)
- pka
- 10.12±0.15(Predicted)
- form
- Solid
- color
- White to off-white
Safety
- HS Code
- 2935909099
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-6243
- Product name
- AMG-3969
- Purity
- 99.74%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- BISN0048
- Product name
- AMG-3969
- Purity
- 99%
- Packaging
- 5mg
- Price
- $522
- Updated
- 2021/12/16
- Product number
- CS-6243
- Product name
- AMG-3969
- Purity
- 99.74%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- BISN0048
- Product name
- AMG-3969
- Purity
- 99%
- Packaging
- 10mg
- Price
- $747
- Updated
- 2021/12/16
- Product number
- CS-6243
- Product name
- AMG-3969
- Purity
- 99.74%
- Packaging
- 1mg
- Price
- $180
- Updated
- 2021/12/16
AMG-3969 Chemical Properties,Usage,Production
Description
AMG-3969is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor. Itcan strongly boost the dissociation of the GK-GKRP complex and promote GK translocation in-vivo. In rodent model of diabetes, AMG-3969 reduces blood glucose levels without affecting euglycemic animals. It is a promising drug for the treatment of type II diabetes through lowering blood glucose levels with reduced potential for hypoglycaemic risk.
Uses
AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM.
in vivo
AMG-3969 has good in vivo pharmacokinetic (PK) properties in rats (75%) and significantly lowers blood glucose levels in a dose-dependent manner db/db mice[1]. AMG-3969 (100 mg/kg) demonstrates significant reductions in blood glucose with robust efficacy (56% reduction) observed at the 8 h time point[2]. AMG-3969 demonstrates dose-dependent efficacy in three models of diabetes: diet induced obese (DIO), ob/ob and db/db mice; however,AMG-3969 is ineffective in lowering blood glucose in normoglycaemic C57BL/6 (B6) mice. AMG-3969 is highly effective in promoting carbohydrate substrate. AMG-3969 exhibits extended changes to carbohydrate oxidation as observed by increased respiratory exchange ratio into the next night and day after a single dose[3].
References
Lloyd, David J., et al. "Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors." Nature 504.7480(2013):437-40.
Bourbeau, M. P., et al. "Nonracemic synthesis of GK-GKRP disruptor AMG-3969. " Synfacts 79.8(2014):3684.
http://www.metonchem.com/products/amg-3969-cas1361224-53-4/
AMG-3969 Preparation Products And Raw materials
Raw materials
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