AMG-3969

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mg
ArtNr HY-12411-10mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Synonyms
AMG3969, AMG 3969
CAS No.
1361224-53-4
Purity
>98%
MW
5224639
Formula
C21H20F6N4O3S
Solubility
10 mM in DMSO
Biological Description
AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM.
IC50 & Target: IC50: 4 nM (GK-GKRP)[1]
In Vitro: AMG-3969 exhibits potent cellular activity with an EC50 of 0.202 uM 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].
Menge: 10mg
Lieferbar: In stock
Listenpreis: 636,07 €
Rabatt: -10,0%
Preis: 572,46 €
Sie sparen: 63,61 €
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