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BPRPT0245

Chemical Structure : BPRPT0245

CAS No.: 2982603-10-9

BPRPT0245

货号: PC-24307Not For Human Use, Lab Use Only.

BPRPT0245 is a specific small-molecule inhibitor of prostaglandin reductase 2 (PTGR2) with IC50 of 8.92 nM, restores 15-keto-PGE2-dependent PPARγ trans-activation in HEK293T cells expressing recombinant PTGR2 with EC50 of 49.22 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BPRPT0245 is a specific small-molecule inhibitor of prostaglandin reductase 2 (PTGR2) with IC50 of 8.92 nM, restores 15-keto-PGE2-dependent PPARγ trans-activation in HEK293T cells expressing recombinant PTGR2 with EC50 of 49.22 nM.
BPRPT0245 not only increased intracellular 15-keto-PGE2 concentrations in a dose-dependent manner but also augmented insulin-stimulated glucose uptake of differentiated 3T3-L1 adipocytes.
BPRPT0245 interferes with the interaction between 15-keto-PGE2 and NADPH within the catalytic site of hPTGR2.
BPRPT0245 protected mice from diet-induced obesity, insulin resistance, glucose intolerance, and fatty liver without fluid retention and reduced bone density.

物理化学性质&存储条件

分子量 446.53
分子式 C25H27FN6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(4-fluorobenzyl)-5-methyl-2-(1-(4-phenylpiperazin-1-yl)ethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7(4H)-one

参考文献

1. Chang YC, et al. EMBO Mol Med. 2025 Mar 21. doi: 10.1038/s44321-025-00216-4.

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