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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-TP-18
TP-18

Chemical Structure : TP-18

CAS No.:

TP-18 (TP18, EP2/EP4 antagonist)

货号: PC-27006Not For Human Use, Lab Use Only.

TP-18 is a potent, selective, orally available dual PGE2 receptor EP2/EP4 antagonist with IC50 of 9.5/3.3 nM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

TP-18 is a potent, selective, orally available dual PGE2 receptor EP2/EP4 antagonist with IC50 of 9.5/3.3 nM respectively.
TP-18 potently suppressed PGE2-induced β-arrestin recruitment in CHO-EP2 cells and CHO-EP4 cells with IC50 values of 11.1 and 10.5 nM, respectively.
TP-18 displays robust antagonism against EP2 and EP4 in GPCR assay based on Gα16-mediated calcium flux, with high selectivity of >1,000-fold against the EP1 and EP3 receptors.
TP-18 physically occupies the PGE2-binding pockets of EP2 and EP4 structures.
TP-18 triggers CD8+ T cell-mediated anti-tumor immune response to promote tumor regression, demonstrates superior anti-tumor efficacy compared to EP2i, EP4i, and celecoxib.
TP-18 boosts CD8+ T cell response via depleting immunosuppressive VSIG4high tumor-associated macrophages (TAMs).
TP-18 impairs expression of immune checkpoint molecule VSIG4 in TAMs through inactivating Gαs-PKA-CREB signaling.
TP-18 overcomes primary and acquired resistance to anti-PD-1 therapy in colorectal cancer models, improves the efficacy of anti-PD-1 therapy in patient-derived tumor immune organoids.

物理化学性质&存储条件

分子量 448.50
分子式 C25H25FN4O3
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

2-ethoxy-4-(6-((2-(7-fluoro-2,4-dimethyl-1H-indol-3-yl)ethyl)amino)pyrimidin-4-yl)benzoic acid

参考文献

1. Zhang Y, et al. Cell Rep. 2026 May 28;45(6):117450.

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