| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 70 nM (GPR4). | ||||||||||||
| Invitro | NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation (IC50 26.8 nM in HEK293 cells)[2]. | ||||||||||||
| 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: | ||||||||||||
| Name | NE 52-QQ57 | ||||||||||||
| CAS | 1401728-56-0 | ||||||||||||
| Formula | C24H28N6O | ||||||||||||
| Molar Mass | 416.52 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [2]. Hosford PS, et al. CNS distribution, signalling properties and central effects of G-protein coupled receptor 4. Neuropharmacology. 2018 Aug;138:381-392. |
NE 52-QQ57
CAS: 1401728-56-0 F: C24H28N6O W: 416.52
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory
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