ChemicalBook--->CAS DataBase List--->2253744-53-3

2253744-53-3

2253744-53-3 Structure

2253744-53-3 Structure
IdentificationBack Directory
[Name]

DJ-V159
[CAS]

2253744-53-3
[Synonyms]

DJ-V159
DJ-V159;DJ-V 159
1,3-Benzenedicarboxamide, N1,N3-bis[4-cyano-3-(trifluoromethyl)phenyl]-
[EINECS(EC#)]

604-604-1
[Molecular Formula]

C24H12F6N4O2
[MOL File]

2253744-53-3.mol
[Molecular Weight]

502.37
Chemical PropertiesBack Directory
[storage temp. ]

RT
[solubility ]

Soluble in DMSO (up to 60 mg/ml).
[form ]

solid
[color ]

Off-white
[Stability:]

Stable for 2 years from date of purchase? as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Hazard InformationBack Directory
[Description]

GPRC6A? is the receptor for osteocalcin as well as structurally unrelated ligands including L-amino acids, cations and anabolic steroids.1?GPRC6A is a potential therapeutic target for treating type 2 diabetes.2 DJ-V 159 (2253744-53-3) is an agonist at GPRC6A which activates ERK and upregulates cAMP levels in HEK-193 cells expressing GPRC6A. It stimulates insulin secretion in mouse β-cells and lowers blood glucose in mouse models.3
[Uses]

DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
[in vivo]

DJ-V-159 at the dose of 10 mg/kg reduces blood glucose levels in wildtype mice at 60 and 90 minutes after intraperitoneal administration of 10 mg/kg, whereas the vehicle (95% PEG + 5% DMSO) has no effect on blood glucose. DJ-V-159 reduces blood glucose levels in wild-type mice by 43.6% and 41.9% at 60 and 90 minutes, respectively, after intraperitoneal administration of 10 mg/kg. The mice tolerated this short-term exposure to DJ-V-159 without any overt side-effects. DJ-V-159, however, is almost in or on the boundary of the Lipinski's Rule of Five[1].

[storage]

Store at -20°C
[References]

1) Pi and Quarles (2012),?Multiligand specificity and wide tissue expression of GPRC6A reveals new endocrine networks; Endocrinology,?153?2062 2) Pi?et al.?(2016),?GPRC6A: Jack of all metabolism (or master of none); Mol. Metab.,?6?185 3) Pi?et al.?(2018),?Computationally identified novel agonists for GPRC6A; PLoS One,?13?e0195980
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