For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>AR231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release; Antidiabetic agent.<br>IC50 value:<br>Target: GPR119<br>in vitro: The GPR119-specific agonist AR231453 significantly increased cAMP accumulation and insulin release in both HIT-T15 cells and rodent islets. In both cases, loss of GPR119 rendered AR231453 inactive [1]. In GLUTag cells, a well-established model of intestinal L-cell function, the potent GPR119 agonist AR231453 stimulated cAMP accumulation and GLP-1 release [2].<br>in vivo: AR231453 also enhanced glucose-dependent insulin release in vivo and improved oral glucose tolerance in wild-type mice but not in GPR119-deficient mice. Diabetic KK/A(y) mice were also highly responsive to AR231453. Orally active GPR119 agonists may offer significant promise as novel antihyperglycemic agents acting in a glucose-dependent fashion [1]. When administered in mice, AR231453 increased active GLP-1 levels within 2 min after oral glucose delivery and substantially enhanced total glucose-dependent insulinotropic peptide levels. Blockade of GLP-1 receptor signaling with exendin(9-39) reduced the ability of AR231453 to improve glucose tolerance in mice [2].</p>
Catalog Number | I004729 |
CAS Number | 733750-99-7 |
Molecular Formula | C21H24FN7O5S |
Purity | ≥95% |
Target | Neuronal Signaling |
Solubility | 10 mM in DMSO |
Storage | Store at -20C |
InChI | InChI=1S/C21H24FN7O5S/c1-12(2)18-26-21(34-27-18)13-6-8-28(9-7-13)20-17(29(30)31)19(23-11-24-20)25-16-5-4-14(10-15(16)22)35(3,32)33/h4-5,10-13H,6-9H2,1-3H3,(H,23,24,25) |
InChIKey | DGBKNTVAKIFYNU-UHFFFAOYSA-N |
SMILES | O=[N+](C1=C(N2CCC(C3=NC(C(C)C)=NO3)CC2)N=CN=C1NC4=CC=C(S(=O)(C)=O)C=C4F)[O-] |
Reference | <p style=/line-height:25px/> |