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MedKoo CAT#: 555760
CAS#: 2253744-53-3
Description: DJ-V-159 is a novel small molecule agonist of GPRC6A, dose-dependently stimulates cAMP production in GPRC6A expressing HEK-293 cells at 0.2 nM. DJ-V-159 demonstrated the greatest potency in stimulating insulin secretion in β-cells and lowering serum glucose in wild-type mice.
MedKoo Cat#: 555760
Name: DJ-V-159
CAS#: 2253744-53-3
Chemical Formula: C24H12F6N4O2
Exact Mass: 502.0864
Molecular Weight: 502.3764
Elemental Analysis: C, 57.38; H, 2.41; F, 22.69; N, 11.15; O, 6.37
Synonym: DJ-V-159; DJ-V 159; DJ-V159; DJV-159; DJV 159; DJV159;
IUPAC/Chemical Name: N1,N3-Bis(4-cyano-3-(trifluoromethyl)phenyl)isophthalamide
InChi Key: VEVNLJLJLVESLL-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H12F6N4O2/c25-23(26,27)19-9-17(6-4-15(19)11-31)33-21(35)13-2-1-3-14(8-13)22(36)34-18-7-5-16(12-32)20(10-18)24(28,29)30/h1-10H,(H,33,35)(H,34,36)
SMILES Code: O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)C2=CC=CC(C(NC3=CC=C(C#N)C(C(F)(F)F)=C3)=O)=C2
New insights into G protein coupled receptor regulation of glucose metabolism by β-cells, skeletal muscle and liver hepatocytes identify GPRC6A as a potential therapeutic target for treating type 2 diabetes mellitus (T2D). Activating GPRC6A with a small molecule drug represents a potential paradigm-shifting opportunity to make significant strides in regulating glucose homeostasis by simultaneously correcting multiple metabolic derangements that underlie T2D, including abnormalities in β-cell proliferation and insulin secretion and peripheral insulin resistance.
Pi M, Kapoor K, Ye R, et al. Computationally identified novel agonists for GPRC6A. PLoS One. 2018;13(4):e0195980. Published 2018 Apr 23. doi:10.1371/journal.pone.0195980
