TXA₂/TP Modulator

BM-573 is an orally active dual thromboxane A₂ (TXA₂) modulator with an IC₅₀ of 1.3 nM. BM-573 possesses both thromboxane synthase (TxAS) inhibition and thromboxane receptor (TP) antagonistic effects. BM-573 can completely inhibit platelet aggregation induced by Arachidonic acid (HY-109590) or U-46619 (TXA₂ analogues). BM-573 completely blocks the generation of TXB₂ (the stable metabolite of TXA₂) in human platelets and does not inhibit cyclooxygenase (COX-1/COX-2), thus avoiding interference with other prostaglandin synthesis. BM-573 has an inhibitory effect on U-46619-induced contractions in rat gastric fundus smooth muscle (ED₅₀ = 4.2 μM), but has no effect on contractions caused by PGE₂, PGF₂α, or PGI₂. BM-573 can be used in the study of atherosclerosis, myocardial infarction, pulmonary hypertension and shock.

Deacetyltanghinin is a selective inhibitor targeting Na⁺/K⁺ ATPase, acting through non-covalent binding but is highly cardiotoxic. Deacetyltanghinin inhibits Na⁺/K⁺ ATPase activity, induces cancer cell apoptosis (involving caspase pathway activation), and at the same time affect the TXA2-PGI2 balance in the rabbit heart. Deacetyltanghinin has significant anti-cancer activity and is mainly used in the research field of targeted therapy of malignant tumors such as breast cancer and lung cancer. At the same time, attention should be paid to the regulation of its cardiotoxicity.