2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole
- 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
- CAS No.
- 1401728-56-0
- Chemical 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
- GPR4 antagonist 3;NE 52-QQ57 ，S6850;NE 52-QQ57, 10 mM in DMSO;GPR4 antagonist 3(NE 52-QQ57 );inhibit,NE 52 QQ57,NE 52-QQ-57,NE 52-QQ57,NE 52QQ57,Inhibitor;2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole;Pyrazolo[1,5-a]pyrimidine, 2-ethyl-5,7-dimethyl-3-[[4-[5-(4-piperidinyl)-1,3,4-oxadiazol-2-yl]phenyl]methyl]-
- CBNumber
- CB74658413
- Molecular Formula
- C24H28N6O
- Formula Weight
- 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 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- DC20076
- Product name
- GPR4antagonist3(NE52-QQ57)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $800
- Updated
- 2021/12/16
- Product number
- DC20076
- Product name
- GPR4antagonist3(NE52-QQ57)
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1500
- Updated
- 2021/12/16
- Product number
- DC20076
- Product name
- GPR4antagonist3(NE52-QQ57)
- Purity
- >98%
- Packaging
- 1g
- Price
- $3000
- Updated
- 2021/12/16
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,Usage,Production
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
Raw materials
Preparation Products
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