AMG-3969

Alias: AMG-3969; AMG 3969; AMG3969
Cat No.:V2904 Purity: ≥98%
AMG-3969 is a potent, novelandmetabolically stabledisruptor of glucokinase-glucokinase regulatory protein interaction (GK-GKRP) with IC50of 4 nM.
AMG-3969 Chemical Structure CAS No.: 1361224-53-4
Product category: Glucokinase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

AMG-3969 is a potent, novel and metabolically stable disruptor of glucokinase-glucokinase regulatory protein interaction (GK-GKRP) with IC50 of 4 nM. AMG-3969 exhibits potent cellular activity with an EC50 of 0.202 μM and IC50 of 4 nM. It potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation in vitro (isolated hepatocytes). When administered to db/db mice, AMG-3969 demonstrated a robust pharmacodynamic response (GK translocation) as well as statistically significant dose-dependent reductions in fed blood glucose levels. Furthermore, with AMG-1694 and AMG-3969 (but not GK activators), blood glucose lowering was restricted to diabetic and not normoglycaemic animals. These findings exploit a new cellular mechanism for lowering blood glucose levels with reduced potential for hypoglycaemic risk in patients with type II diabetes mellitus.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Strong cellular activity is demonstrated by AMG-3969, which has an EC50 of 0.202 μM and an IC50 of 4 nM[1], [2]. In vitro (isolated hepatocytes), it effectively counteracts the inhibitory effect of GKRP on GK activity and stimulates GK translocation[3].
ln Vivo
According to research, AMG-3969 significantly lowers blood glucose levels in db/db mice in a dose-dependent manner and exhibits good in vivo pharmacokinetic (PK) properties in rats (75%). Blood glucose levels are significantly lowered by AMG-3969 (100 mg/kg), with a strong efficacy (56% reduction) seen at the 8-hour mark[2]. In three diabetes models—diet-induced obese (DIO), ob/ob, and db/db mice—AMG-3969 shows dose-dependent efficacy. In normoglycaemic C57BL/6 (B6) mice, however, AMG-3969 is ineffective in lowering blood glucose. When it comes to promoting carbohydrate substrate, AMG-3969 is very effective. After a single dosage, AMG-3969 shows prolonged changes to carbohydrate oxidation, as evidenced by an increased respiratory exchange ratio into the following day and night[3].
Animal Protocol
Formulated in 2% hydroxypropyl methycellulose, 1% Tween 80, pH 2.2 adjusted with MSA; 10, 30, 100 mg/kg; P.O.
Diet induced obese (DIO), ob/ob and db/db mice
References
[1]. Lloyd DJ, et al. Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors. Nature. 2013 Dec 19;504(7480):437-40.
[2]. Nishimura N, et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series. J Med Chem. 2014 Apr 10;5
[3]. St Jean DJ Jr, et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J Med Chem. 2014 Jan 23;57(2):325-38
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H20F6N4O3S
Molecular Weight
522.46
CAS #
1361224-53-4
SMILES
CC#C[C@@H]1N(C2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)CCN(S(=O)(C3=CN=C(N)C=C3)=O)C1
Synonyms
AMG-3969; AMG 3969; AMG3969
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:10 mM in DMSO
Water:<1 mg/mL
Ethanol:
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9140 mL 9.5701 mL 19.1402 mL
5 mM 0.3828 mL 1.9140 mL 3.8280 mL
10 mM 0.1914 mL 0.9570 mL 1.9140 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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