CGS15435是一种有效的血栓烷(TxA2)合成酶抑制剂，IC50为1nM，比作用于环氧合酶，PGI2合成酶和脂氧合酶的选择性高100000倍。
CAS：95853-92-2
分子式：C20H21ClN2O2
分子量：356.85
纯度：98%
存储：Store at -20°C

Background:

CGS 15435, a potent thromboxane (TxA2) synthetase inhibitor with an IC50 of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI2 synthetase and lipoxygenase enzymes.

CGS 15435 is a highly specific Tx synthetase inhibitor. CGS 15435 is only weakly effective as an inhibitor of PGE2 (Cyclooxygenase, IC50=1200 μM), prostacyclin (PGI2 synthetase, IC50=90 μM) or 5-Lipoxygenase (IC50=60 μM) product formation[1].

CGS 15435 has a long duration of action, since the increases in the plasma levels of TxB2 are prevented even at 24 h after CGS 15435 administration. CGS 15435 significantly inhibits TxB2 formation 4, 6, 12 and 24 h after dosing. Administration of CGS 15435 0.25 or 24 h prior to Arachidonic acid (AA) produced no increase in TxB2 in the surviving animals (4/4 and 5/6, respectively). The final TxB2 levels in the CGS15435A (0.25 and 24 h pretreatment) groups are significantly lower (P<0.05) than those seen in the AA or the Dazoxiben (2 h pretreatment) groups[1].

[1]. Olson RW, et al. CGS 15435A, a thromboxane synthetase inhibitor with an extended duration of action: a comparison with dazoxiben. Eur J Pharmacol. 1987 Jan 20;133(3):265-73.