AMG-3969
Modify Date: 2025-08-25 12:04:45
AMG-3969 structure
|
Common Name | AMG-3969 | ||
|---|---|---|---|---|
| CAS Number | 1361224-53-4 | Molecular Weight | 522.464 | |
| Density | 1.6±0.1 g/cm3 | Boiling Point | 648.8±65.0 °C at 760 mmHg | |
| Molecular Formula | C21H20F6N4O3S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 346.2±34.3 °C | |
Use of AMG-3969AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM. |
| Name | 2-{4-[(2S)-4-[(6-Amino-3-pyridinyl)sulfonyl]-2-(1-propyn-1-yl)-1-piperazinyl]phenyl}-1,1,1,3,3,3-hexafluoro-2-propanol |
|---|---|
| Synonym | More Synonyms |
| Description | AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 4 nM (GK-GKRP)[1] |
| In Vitro | AMG-3969 exhibits potent cellular activity with an EC50 of 0.202 μM and IC50 of 4 nM[1], [2]. It potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation in vitro (isolated hepatocytes)[3]. |
| 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]. |
| Animal Admin | Mice: Diabetic db/db mice are used in the study. At 8:00 AM, mice are bled via retro-orbital sinus puncture and blood glucose values are determined and used to randomize the animals in which their averages are similar, and only mice with blood glucose ranges between 300 and 500 mg/dL are included. Vehicle (2% hydroxypropyl methycellulose, 1% Tween 80, pH 2.2 adjusted with MSA) or AMG-3969 (10, 30, 100 mg/kg) are gavaged at 9:00 AM. Blood glucose is measured at 4, 6, or 8 h posttreatment. At each time point, a 15 μL sample of whole blood is analyzed for drug exposure[2]. |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 648.8±65.0 °C at 760 mmHg |
| Molecular Formula | C21H20F6N4O3S |
| Molecular Weight | 522.464 |
| Flash Point | 346.2±34.3 °C |
| Exact Mass | 522.116028 |
| LogP | 4.51 |
| Vapour Pressure | 0.0±2.0 mmHg at 25°C |
| Index of Refraction | 1.598 |
| InChIKey | SIFKNECWLVONIH-INIZCTEOSA-N |
| SMILES | CC#CC1CN(S(=O)(=O)c2ccc(N)nc2)CCN1c1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1 |
| Storage condition | -20℃ |
|
Name: Oral bioavailability in Sprague-Dawley rat at 10 mg/kg
Source: ChEMBL
Target: Rattus norvegicus
External Id: CHEMBL3240706
|
|
Name: Induction of GK translocation from nucleus to cytoplasm of mouse hepatocytes preincub...
Source: ChEMBL
Target: Hexokinase-4
External Id: CHEMBL3119630
|
|
Name: Half life in Sprague-Dawley rat at 2 mg/kg, iv
Source: ChEMBL
Target: Rattus norvegicus
External Id: CHEMBL3240705
|
|
Name: Inhibition of fluorescein-labeled human GK interaction with biotin-labeled human GKRP...
Source: ChEMBL
Target: Hexokinase-4
External Id: CHEMBL3117036
|
|
Name: Clearance in C57BL/6 mouse at 2 mg/kg, iv
Source: ChEMBL
Target: Mus musculus
External Id: CHEMBL3240708
|
|
Name: AUC in Sprague-Dawley rat at 10 mg/kg, po
Source: ChEMBL
Target: Rattus norvegicus
External Id: CHEMBL3240707
|
|
Name: Oral bioavailability in C57BL/6 mouse at 10 mg/kg
Source: ChEMBL
Target: Mus musculus
External Id: CHEMBL3240710
|
|
Name: Half life in C57BL/6 mouse at 2 mg/kg, iv
Source: ChEMBL
Target: Mus musculus
External Id: CHEMBL3240709
|
|
Name: Experimentally measured binding affinity data (IC50) for protein-ligand complexes der...
Source: Shanghai Institute of Organic Chemistry
Target: N/A
External Id: PDBbind-IC50 for protein-ligand complexes
|
|
Name: AUC in C57BL/6 mouse at 10 mg/kg, po
Source: ChEMBL
Target: Mus musculus
External Id: CHEMBL3240711
|
Total 33, Current Page 1 of 4
1
2
3
4
| 2-{4-[(2S)-4-[(6-Amino-3-pyridinyl)sulfonyl]-2-(1-propyn-1-yl)-1-piperazinyl]phenyl}-1,1,1,3,3,3-hexafluoro-2-propanol |
| AMG-3969 |