AR 231453

Research use only, not for human use.

AR 231453 is a selective and orally available GPR119 agonistcan stimulate β-cell replication and improve islet graft function.

AR 231453 is a selective and orally available GPR119 agonistcan stimulate β-cell replication and improve islet graft function.

AR 231453 is inactive at all other GPCRs tested (more than 230, including all known pancreatic islet receptors), indicating that it is highly selective for GPR119.AR 231453 potently stimulats cAMP accumulation (EC50 = 4.7 nM) with a maximal efficacy similar to that seen with forskolin. AR 231453 significantly enhances insulin release in HIT-T15 cells, with an EC50 of 3.5 nM.AR 231453 also stimulates insulin release in isolated mouse islets at glucose concentrations ranging from 8-17 mM.

AR231453 (20 mg/kg, orally) markedly improves oral glucose tolerance in a dose-dependent fashion, with efficacy similar to maximally effective doses of the sulfonylurea glyburide. Animal Model:Mice.Dosage:20 mg/kg. Administration:Orally, once.Result:Improved glucose tolerance in mice.

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Cell Cycle/DNA Damage

GPR

GPR119

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733750-99-7

505.52

C21H24FN7O5S

>98% (HPLC)

DMSO:60 mg/mL (118.69 mM);H2O:60 mg/mL (118.69 mM; Need ultrasonic and warming)

CC(C)c1noc(n1)C1CCN(CC1)c1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O

N-(2-fluoro-4-methanesulfonylphenyl)-(6-[4-(3-isopropyl-[124]oxadiazol-5-yl)-piperidin-1-yl]-5-nitropyrimidin-4-yl)amine

(-20℃)

With Ice Pack

≥ 2 years