TPST-1495 | EP2/EP4 antagonist | Probechem Biochemicals

Chemical Structure : TPST-1495

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TPST-1495 (TPST1495)

货号: PC-21037Not For Human Use, Lab Use Only.

TPST-1495 (TPST1495) is a potent, selective, orally available dual EP2/EP4 PGE2 receptor antagonist with IC50 of 17.21/3.24 nM, respectively.

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生物&药学活性

TPST-1495 (TPST1495) is a potent, selective, orally available dual EP2/EP4 PGE2 receptor antagonist with IC50 of 17.21/3.24 nM, respectively.
TPST-1495 does not achieve 50% inhibition of EP1 or EP3 receptors at concentrations up to 30 uM.
TPST-1495 rescues production of TNFα by monocytes at both low and high PGE2 concentrations with IC50 values of 1 nmol/L and 382 nmol/L, respectively, overcomes PGE2-mediated immune suppression in mouse and human monocytes in vitro.
TPST-1495 is more effective than a single EP4 or EP2 antagonists (E7046 and PF04419848) in overcoming PGE2-mediated immune suppression of recovery of cytokine production from murine monocytes and T cells.
TPST-1495 (100 mg/kg twice a day, orally) confers therapeutic efficacy in mice bearing PGE2-producing tumors.
TPST-1495 exhibits immune-independent antitumor activity.

物理化学性质&存储条件

分子量
分子式
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

TPST-1495 (TPST1495)

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物理化学性质&存储条件

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TPST-1495 (TPST1495)

生物&药学活性

物理化学性质&存储条件

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