DJ-V159( —— )

Catalog No. M19914 CAS No. 2253744-53-3

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Product Name

DJ-V159
Note

Research use only, not for human use.
Brief Description

DJ-V159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
Description

DJ-V159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
In Vitro

DJ-V-159 activates ERK in HEK-293 transfected with GPRC6A but not in non-transfected HEK-293 cells, with potency similar to L-Arg. In addition, DJ-V-159 dose-dependently stimulates cAMP production in GPRC6A expressing HEK-293 cells, achieving a response a 0.2 nM concentrations in the media. DJ-V-159 stimulates insulin secretion in mouse beta-cell MIN-6 cells. The DJ-V-159 increased insulin stimulation index (SI) in MIN-6 cells similar to the effects of Ocn, known ligand of 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.
Synonyms

——
Pathway

Cell Cycle/DNA Damage
Target

GPR
Recptor

GPRC6A
Research Area

——
Indication

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1.Pi M et al. Computationally identified novel agonists for GPRC6A. PLoS One. 2018 Apr 23;13(4):e0195980.

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