SML3643
EP2 antagonist C52
≥98% (HPLC)
别名:
4-((9-Chloro-7-(5-fluoro-1H-indol-1-yl)-2,3-dihydrobenzo[f ]-[1,4]oxazepin-4(5H)-yl)methyl)pyridin-2(1H)-one, 4-[[9-Chloro-7-(5-fluoro-1H-indol-1-yl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl]methyl]-2(1H)-pyridinone, Benzoxazepine 52, C52, Compound 52, EP2 antagonist compound 52
产品名称
EP2 antagonist C52, ≥98% (HPLC)
SMILES string
O=C1C=C(CN2CC3=CC(N4C=CC5=C4C=CC(F)=C5)=CC(Cl)=C3OCC2)C=CN1
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Compound 52 (C52) is an orally active, brain-penetrant, highly potent and selective prostaglandin E2 (PGE2) receptor 2 (EP2) antagonist (h/r/m EP2 IC50 = 8/10/10 nM against PGE2 binding, IC50 = 5/3/4 nM against 10 nM PGE2-induced cellular cAMP) with ∼4000-fold selectivity over other EP receptors (hEP1/3/4 IC50 >30 μM against PGE2 binding; hCRTH2/DP/IP/TP IC50 >33 μM against LTD4-induced cellular Ca2+) and no CYP inhibitory potency. C52 reduces inflammatory neurodegeneration in a murine model of cerebral ischemia (10 mg/kg p.o. 4.5h & 24h post MCAO) and restores cognition in aged mice (10 mg/kg/d p.o.) by rejuvenating cellular bioenergetics in vivo.
Orally active, brain-penetrant, highly potent and selective prostaglandin E2 (PGE2) receptor 2 (EP2) antagonist in vitro and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Brian M Fox et al.
Journal of medicinal chemistry, 58(13), 5256-5273 (2015-06-11)
A high-throughput screen resulted in the discovery of benzoxazepine 1, an EP2 antagonist possessing low microsomal stability and potent CYP3A4 inhibition. Modular optimization of lead compound 1 resulted in the discovery of benzoxazepine 52, a molecule with single-digit nM binding
Qingkun Liu et al.
Proceedings of the National Academy of Sciences of the United States of America, 116(20), 10019-10024 (2019-05-01)
The inflammatory prostaglandin E2 (PGE2) EP2 receptor is a master suppressor of beneficial microglial function, and myeloid EP2 signaling ablation reduces pathology in models of inflammatory neurodegeneration. Here, we investigated the role of PGE2 EP2 signaling in a model of
Paras S Minhas et al.
Nature, 590(7844), 122-128 (2021-01-22)
Ageing is characterized by the development of persistent pro-inflammatory responses that contribute to atherosclerosis, metabolic syndrome, cancer and frailty1-3. The ageing brain is also vulnerable to inflammation, as demonstrated by the high prevalence of age-associated cognitive decline and Alzheimer's disease4-6.
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