Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H24FN5O5S |
Molecular Weight | 477.509 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)OC(=O)N1CCC(CC1)OC2=NC=NC3=C2C=NN3C4=C(F)C=C(C=C4)S(C)(=O)=O
InChI
InChIKey=XTRUQJBVQBUKSQ-UHFFFAOYSA-N
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
APD668 is a novel, highly potent and orally active glucose-dependent insulinotropic receptor (GDIR) agonist intended to more efficiently stimulate insulin release by beta cells in response to elevated blood glucose levels, and to avoid hypoglycemia. Ortho-McNeil's initial clinical studies evaluated healthy volunteers and patients with type 2 diabetes in randomized, double-blind, placebo-controlled trials evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple (14 day) escalating doses of APD668. Based on the data from those studies, Ortho-McNeil has decided to put APD668 on hold and has advanced a potentially more potent Arena discovered GDIR agonist into preclinical development.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5652 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21444206 |
2.7 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21444206
Unknown
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11705608
Created by
admin on Sat Dec 16 11:31:13 GMT 2023 , Edited by admin on Sat Dec 16 11:31:13 GMT 2023
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JC77BCH2AP
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DTXSID701025686
Created by
admin on Sat Dec 16 11:31:13 GMT 2023 , Edited by admin on Sat Dec 16 11:31:13 GMT 2023
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832714-46-2
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admin on Sat Dec 16 11:31:13 GMT 2023 , Edited by admin on Sat Dec 16 11:31:13 GMT 2023
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APD-668
Created by
admin on Sat Dec 16 11:31:13 GMT 2023 , Edited by admin on Sat Dec 16 11:31:13 GMT 2023
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PRIMARY | JNJ-28630368: GPR119, a glucose-dependent insulinotropic receptor, is a G protein-coupled receptor that is expressed in pancreatic .BETA.-cells and intestinal L-cells.1 Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine (Item No. 10172) and oleoyl ethanolamide (Item No. 90265) increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.1,2 APD668 is a potent agonist of GPR119 (EC50s = 2.7 and 33 nM for human and rat forms, respectively).3 Chronic dosing with APD668 in Zucker diabetic fatty rats over several weeks significantly reduces blood glucose and glycated hemoglobin levels. |
ACTIVE MOIETY