| Identification | Back Directory | [Name]
AR 231453 | [CAS]
733750-99-7 | [Synonyms]
CS-2809
AR 231453
AR231453; AR-231453
N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5
N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5-ni
N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5-nitropyrimidin-4-amine
(2-FLUORO-4-METHANESULFONYL-PHENYL)-(6-[4-(3-ISOPROPYL-[1,2,4]OXADIAZOL-5-YL)-PIPERIDIN-1-YL]-5-NITRO-PYRIMIDIN-4-YL)-AMINE
4-Pyrimidinamine, N-[2-fluoro-4-(methylsulfonyl)phenyl]-6-[4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-1-piperidinyl]-5-nitro- | [Molecular Formula]
C21H24FN7O5S | [MDL Number]
MFCD14706714 | [MOL File]
733750-99-7.mol | [Molecular Weight]
505.52 |
| Chemical Properties | Back Directory | [Melting point ]
174-176℃ | [Boiling point ]
703.9±70.0 °C(Predicted) | [density ]
1.421±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 25 mg/ml; DMSO: 3 mg/ml; Ethanol: insol; PBS (pH 7.2): insol | [form ]
Yellow solid. | [pka]
3.24±0.10(Predicted) | [color ]
Light yellow to yellow | [InChIKey]
DGBKNTVAKIFYNU-UHFFFAOYSA-N | [SMILES]
CC(C)C1=NOC(C(CC2)CCN2C(N=CN=C3NC4=CC=C(C=C4F)S(=O)(C)=O)=C3[N+]([O-])=O)=N1 |
| Hazard Information | Back Directory | [Uses]
AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s[1][2]. | [Biological Activity]
AR231453 is a 5-nitropyrimidine derivative th at acts as a highly potent and selective GPR119 agonist (EC50/GPR119 species = 0.4 nM/monkey1.6 nM/dog4.7 nM/hamster3.5 nM/human12 nM/mouse4 nM/r at in cell-based assays)exhibiting no off-target activity toward 216 receptorsenzymesand orphan GPCRs. AR231453 improves glucose tolerance in mice (3 mg/kg i.p. or 20 mg/kgp.o.) and rats (3 mg/kg i.p.)while no in vivo efficacy is observed among GPR119-deficient mice. | [in vivo]
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[1].
| Animal Model: | Mice[1]. | | Dosage: | 20 mg/kg. | | Administration: | Orally, once. | | Result: | Improved glucose tolerance in mice. |
| [References]
[1] Chu ZL, et al. A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. Endocrinology. 2007 Jun;148(6):2601-9. DOI:10.1210/en.2006-1608
[2] J Gao, et al. Stimulating β-cell replication and improving islet graft function by AR231453, A GPR119 agonist. Transplant Proc. 2011 Nov;43(9):3217-20. DOI:10.1016/j.transproceed.2011.10.021 |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|