Identification | Back 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 Properties | Back 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 Information | Back 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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Company Name: |
cjbscvictory
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Tel: |
13348960310 13348960310 |
Website: |
https://www.weikeqi-biotech.com/ |
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