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DJ-V159

SKU: orb1221195

Description

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

Images & Validation

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DJ-V159

Key Properties

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CAS Number2253744-53-3
MW502.37
Purity>98% (HPLC)
FormulaC24H12F6N4O2
SMILESFC(F)(F)c1cc(NC(=O)c2cccc(c2)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F)ccc1C#N
TargetGPR
SolubilityDMSO: 10 mg/mL

Bioactivity

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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.
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.

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Similar Products

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  • DJ-V 159 [orb1302091]

    >98%

    2253744-53-3

    502.4

    C24H12F6N4O2

    5 mg, 25 mg
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Quick Database Links

Gene Symbol
GPR

Protocol Information

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