2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole manufacturers
- NE 52-QQ57
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- $44.00 / 1mg
-
2025-11-10
- CAS:1401728-56-0
- Min. Order:
- Purity: 98.63%
- Supply Ability: 10g
- NE 52-QQ57
-
- $44.00 / 1mg
-
2025-11-10
- CAS:1401728-56-0
- Min. Order:
- Purity: 98.63%
- Supply Ability: 10g
|
| | 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 | | EINECS: | | | Product Categories: | | | 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 Structure](CAS/20200401/GIF/1401728-56-0.gif) |
| | 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 |
| | 2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole Preparation Products And Raw materials |
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