2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole
2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole Basic information
- Product Name:
- 2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole
- Synonyms:
-
- 2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole
- GPR4 antagonist 3
- Pyrazolo[1,5-a]pyrimidine, 2-ethyl-5,7-dimethyl-3-[[4-[5-(4-piperidinyl)-1,3,4-oxadiazol-2-yl]phenyl]methyl]-
- GPR4 antagonist 3(NE 52-QQ57 )
- inhibit,NE 52 QQ57,NE 52-QQ-57,NE 52-QQ57,NE 52QQ57,Inhibitor
- NE 52-QQ57, 10 mM in DMSO
- NE 52-QQ57 ，S6850
- CAS:
- 1401728-56-0
- MF:
- C24H28N6O
- MW:
- 416.52
- Mol File:
- 1401728-56-0.mol
2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole Chemical Properties
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:10.0(Max Conc. mg/mL);24.1(Max Conc. mM)
Ethanol:45.0(Max Conc. mg/mL);108.0(Max Conc. mM) - form
- Solid
- pka
- 9.56±0.10(Predicted)
- color
- White to yellow
2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole Usage And Synthesis
Uses
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity[1].
in vivo
NE 52-QQ57 (Compound 13) shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid for 20 days[1]. NE 52-QQ57 (30 mg/kg bid po for 4 days) also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund’s adjuvant model[1].
| Animal Model: | Female FVB mice (8-10 weeks)[1] |
| Dosage: | 30 mg/kg |
| Administration: | Oral, 4 days, bid |
| Result: | Treatment at 30 mg/kg p.o. bid starting on day 0, the day of the chamber implantation, showed a statistically significant reduction (46.8±10.6%) of tissue growth by day 4. The blood levels of 13 on day 4 at 2 and 16 h after compound application in this model were 9.03±2.87 and 0.09±0.06 μM[1]. |
| Animal Model: | Male Wistar Han rats[1] |
| Dosage: | 3, 10, and 30 mg/kg |
| Administration: | Oral, 20 days, bid |
| Result: | Displayed not only higher exposures in the rat AIA but also lower plasma protein binding in rat (95%)[1]. |
References
[1] Velcicky J, et al. Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis. J Med Chem. 2017 May 11;60(9):3672-3683. DOI:10.1021/acs.jmedchem.6b01703
[2] Hosford PS, et al. CNS distribution, signalling properties and central effects of G-protein coupled receptor 4. Neuropharmacology. 2018 Aug;138:381-392. DOI:10.1016/j.neuropharm.2018.06.007
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