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Chemical Structure : AR231453
CAS No.: 733750-99-7
Catalog No.: PC-20426Not For Human Use, Lab Use Only.
AR231453 (AR 231453) is the first potent, selective and orally efficacious GPR119 agonist with EC50 of 0.68 nM.
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|---|---|---|---|
| 25 mg | $198 | In stock | |
| 100 mg | $498 | In stock | |
| 200 mg | $758 | In stock | |
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AR231453 (AR 231453) is the first potent, selective and orally efficacious GPR119 agonist with EC50 of 0.68 nM.
AR231453 displays no off-target activity across a 76 receptor and enzyme profiling panel (CEREP).
AR231453 has activity across species, albeit with somewhat lower potency in rodents (EC50 monkey GPR119=0.4 nM; mouse GPR119 =12 nM; rat GPR119=14 nM; dog GPR119=1.6 nM).
AR231453 stimulates cAMP production via endogenously expressed GPR119 in the β-cell like hamster insulinoma line HIT-T15 with IC50 of 4.7 nM.
AR231453 (20 mg/kg, po) enhanced glucose-dependent insulin release and improved oral glucose tolerance in wild-type C57/bl6J mice but not in GPR119-deficient mice.
| M.Wt | 505.53 | |
| Formula | C21H24FN7O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(2-fluoro-4-methanesulfonylphenyl)-(6-[4-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-piperidin-1-yl]-5-nitropyrimidin-4-yl)amine |
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1. Semple G, et al. J Med Chem. 2008 Sep 11;51(17):5172-5.
2. Chu ZL, et al. Endocrinology. 2008 May;149(5):2038-47.
3. Chu ZL, et al. Mol Endocrinol. 2010 Jan;24(1):161-70.
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