产品
编 号：F539848
分子式：C20H21ClN2O2
分子量：356.85
分子式：C20H21ClN2O2
分子量：356.85
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CAS No: 95853-92-2
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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.
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.
体内研究：
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.
体外研究：
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.
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