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JNJ-38431055

Names

[ CAS No. ]:
897732-93-3

[ Name ]:
JNJ-38431055

[Synonym ]:
adp-597
Isopropyl 4-[(5-methoxy-6-{[2-methyl-6-(methylsulfonyl)-3-pyridinyl]amino}-4-pyrimidinyl)oxy]-1-piperidinecarboxylate
1-Piperidinecarboxylic acid, 4-[[5-methoxy-6-[[2-methyl-6-(methylsulfonyl)-3-pyridinyl]amino]-4-pyrimidinyl]oxy]-, 1-methylethyl ester
JNJ-38431055
APD597

Biological Activity

[Description]:

APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.IC50 value: 46 nM (EC50) [1]Target: hGPR119The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. APD597 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. [1]

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GPR119
Research Areas >> Metabolic Disease

[References]

[1]. Buzard DJ, et al. Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-4335.

[2]. Semple G, et al. Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improvedprofile. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-1755.

[3]. Huan Y, et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017 Jun 28;7(1):4351.


[Related Small Molecules]

AR 231453 | MBX-2982 | PSN632408 | GSK1292263 | APD 668 | Firuglipel

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
648.3±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H29N5O6S

[ Molecular Weight ]:
479.550

[ Flash Point ]:
345.9±31.5 °C

[ Exact Mass ]:
479.183868

[ PSA ]:
141.22000

[ LogP ]:
2.90

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.570

[ Storage condition ]:
-20℃

Related Compounds