AR231453 | GPR119 agonist | Probechem Biochemicals

Chemical Structure : AR231453

CAS No.: 733750-99-7

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AR231453 (AR 231453)

货号: 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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10 mg	￥880	In stock
25 mg	￥1380	In stock
50 mg	￥2180	In stock
100 mg	￥3280	In stock
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	505.53
分子式	C21H24FN7O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

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.

AR231453 (AR 231453)

生物&药学活性

物理化学性质&存储条件

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AR231453 (AR 231453)

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物理化学性质&存储条件

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