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APD 668
- JNJ 28630368
Axon 2380
CAS:
832714-46-2
Purity:
100%
- Soluble in DMSO
- MF: C21H24FN5O5S
- MW: 477.51
Description
Potent and selective, orally active G protein-coupled receptor 119 agonist (EC50 values 2.7 nM and 23 nM for hGPR119 and rGPR119, respectively) with in vivo activity in rodent models of glucose control. APD 668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat.
APD 668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM).
More Information
| Parent CAS No. | 832714-46-2 |
|---|---|
| Chemical Name | isopropyl 4-(1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate |
| SMILES | N1(C(OC(C)C)=O)CCC(OC2N=CN=C3N(C4=CC=C(S(C)(=O)=O)C=C4F)N=CC3=2)CC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C21H24FN5O5S/c1-13(2)31-21(28)26-8-6-14(7-9-26)32-20-16-11-25-27(19(16)23-12-24-20)18-5-4-15(10-17(18)22)33(3,29)30/h4-5,10-14H,6-9H2,1-3H3 |
| InChiKey | XTRUQJBVQBUKSQ-UHFFFAOYSA-N |
| CID | 11705608 |
| Short Description | GPR119 agonist |
References
- G. Semple et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg. Med. Chem. Lett. 2011, 21, 3134-3141.
- M. Sakairi et al. Synthesis and pharmacological profile of a new selective G protein-coupled receptor 119 agonist; 6-((2-fluoro-3-(1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)propyl)amino)-2,3-dihydro-.... Chem. Pharm. Bull. 2012, 60, 1093-1095.
- E. Weisberg et al. Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells. PLoS One. 2013, 8, e56473.
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