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AR 231453
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AR 231453图片
CAS NO:733750-99-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
500mg电议
1g电议

产品介绍
AR 231453 是一种有效、特异性和可口服的 GPR119 激动剂。
Cas No.733750-99-7
化学名N-(2-fluoro-4-methylsulfonylphenyl)-5-nitro-6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]pyrimidin-4-amine
Canonical SMILESCC(C)C1=NOC(=N1)C2CCN(CC2)C3=C(C(=NC=N3)NC4=C(C=C(C=C4)S(=O)(=O)C)F)[N+](=O)[O-]
分子式C21H24FN7O5S
分子量505.52
溶解度≥ 49.3 mg/mL in DMSO with gentle warming
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AR 231453 is an agonist of GPR119 with EC50 value of 0.68nM [1].

AR 231453 is the first subnanomolar agonist of GPR119. It is highly selective against GPR119 over a 76 receptor and enzyme profiling panel (CEREP) including the known incretin receptors. It also has no activity to 140 known and orphan GPCRs in melanophore dispersion assays. Besides that, AR 231453 is reported to stimulate cAMP production via endogenously expressed GPR119 in HIT-T15 cell line with EC50 value of 4.7nM [1].

In vivo assay shows that AR 231453 has activity in rodents. It can enhance glucose-dependent insulin release and improve oral glucose tolerance in wild-type C57/bl6J mice but not in GPR119-deficient mice at a dose of 20 mg/kg. Due to its activity to active GPR119, AR 231453 is expected to be a potent anti-diabetic agent [1].

References:
[1] Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Choi K, Xiong Y, Ren A, Morgan M, Dave V, Thomsen W, Unett DJ, Xing C, Bossie S, Carroll C, Chu ZL, Grottick AJ, Hauser EK, Leonard J, Jones RM. Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. J Med Chem. 2008 Sep 11;51(17):5172-5.