L001 | EP4 antagonist | Probechem Biochemicals

Chemical Structure : L001

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L001 (EP4 antagonist L001)

货号: PC-20855Not For Human Use, Lab Use Only.

L001 is a potent and selective EP4 antagonist with cAMP IC50 of 7.29 nM, impairs pancreatic cancer migration and invasion.

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生物&药学活性

L001 is a potent and selective EP4 antagonist with cAMP IC50 of 7.29 nM, impairs pancreatic cancer migration and invasion.
L001 is superior to E7046 in CRE reporter assay (IC50=40.6 nM).
L001 blocks PGE2-induced EP4/β-arrestin2 interaction with an IC50 value of 0.16 nM in TANGO assay, significantly blocks the PGE2-induced phosphorylation of ERK1/2 in a dose-dependent manner.
L001 exhibits a >600-fold greater selectivity in human EP4 than the other prostaglandin E receptors (IC50 > 10 µM for EP1, EP2 and EP3).
L001 is a potent EP4 antagonist in human, monkey, mouse and rat as detected by the calcium flux assay with IC50 values of 1.47 nM, 5.24 nM, 3.20 nM and 14.25 nM, respectively.
L001 (10 uM) affects PGE2-induced pancreatic cancer cell migration using the wound healing assay and transwell assay.
L001 abrogates Hippo-YAP activation and pro-metastatic factors expression in pancreatic cancer cells.
L001 treatment (75 mg/kg/day) impairs hepatic metastasis of pancreatic cancer in vivo.

物理化学性质&存储条件

分子量	489.51
分子式	C25H22F3NO4S
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	O=C(N[C@H](C1=CC=C(C(O)=O)C=C1)C)C2=C(CC3=CC=CC(C(F)(F)F)=C3)SC4=C2CCOC4

参考文献

1. Jiacheng He, et al. Molecules. 2022 Feb 11;27(4):1209.

L001 (EP4 antagonist L001)

生物&药学活性

物理化学性质&存储条件

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L001 (EP4 antagonist L001)

生物&药学活性

物理化学性质&存储条件

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