DJ-V-159 | CAS#2253744-53-3 | GPRC6A agonist

MedKoo Cat#: 555760 | Name: DJ-V-159

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

DJ-V-159

CAS#2253744-53-3

Theoretical Analysis

MedKoo Cat#: 555760

Name: DJ-V-159

CAS#: 2253744-53-3

Chemical Formula: C24H12F6N4O2

Exact Mass: 502.0864

Molecular Weight: 502.38

Elemental Analysis: C, 57.38; H, 2.41; F, 22.69; N, 11.15; O, 6.37

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 1,950.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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Related CAS #

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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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

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.

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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

In vitro activity:

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 (Fig 5B). In addition, DJ-V-159 dose-dependently stimulated cAMP production in GPRC6A expressing HEK-293 cells, achieving a response a 0.2 nM concentrations in the media (Fig 5C). Reference: PLoS One. 2018 Apr 23;13(4):e0195980. https://pubmed.ncbi.nlm.nih.gov/29684031/

In vivo activity:

DJ-V-159 at the dose of 10 mg/kg reduced blood glucose levels in wild-type mice at 60 and 90 minutes after intraperitoneal administration of 10 mg/kg (Fig 6B), whereas the vehicle (95% PEG + 5% DMSO) had no effect on blood glucose (Fig 6C). DJ-V-159 reduced 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 (Fig 4B). Reference: PLoS One. 2018 Apr 23;13(4):e0195980. https://pubmed.ncbi.nlm.nih.gov/29684031/

	Solvent	mg/mL	mM
Solubility
	DMSO	15.5	30.85

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 502.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Pi M, Kapoor K, Ye R, Hwang DJ, Miller DD, Smith JC, Baudry J, Quarles LD. Computationally identified novel agonists for GPRC6A. PLoS One. 2018 Apr 23;13(4):e0195980. doi: 10.1371/journal.pone.0195980. PMID: 29684031; PMCID: PMC5912754.

In vitro protocol:

In vivo protocol:

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