ChemicalBook > CAS DataBase List > AMG-3969

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
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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
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Safety

HS Code 
2935909099
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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.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-6243
Product name
AMG-3969
Purity
99.74%
Packaging
5mg
Price
$420
Updated
2021/12/16
Apolloscientific
Product number
BISN0048
Product name
AMG-3969
Purity
99%
Packaging
5mg
Price
$522
Updated
2021/12/16
ChemScene
Product number
CS-6243
Product name
AMG-3969
Purity
99.74%
Packaging
10mg
Price
$600
Updated
2021/12/16
Apolloscientific
Product number
BISN0048
Product name
AMG-3969
Purity
99%
Packaging
10mg
Price
$747
Updated
2021/12/16
ChemScene
Product number
CS-6243
Product name
AMG-3969
Purity
99.74%
Packaging
1mg
Price
$180
Updated
2021/12/16
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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

Preparation Products

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1361224-53-4, AMG-3969Related Search:


  • AMG-3969
  • CS-2503
  • AMG-3969; AMG 3969; AMG3969
  • 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
  • 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
  • AMG-3969, 10 mM in DMSO
  • 1361224-53-4
  • C21H20F6N4O3S