284464-83-1
Chemical Structure
BM-573
- CAS No.: 284464-83-1
- Formula:C18H22N4O5S
- Molecular Weight:406.46
InChIKey: SILRUCMXYIKULW-UHFFFAOYSA-N
SMILES: CC(C)(C)NC(NS(C1=C(NC2=CC=C(C)C=C2)C=CC([N+]([O-])=O)=C1)(=O)=O)=O
Biological Activity: 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[1][2].
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BM-573 | 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. | |||||||||||||||||||||
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- [1]. Ghuysen A, et al. Pharmacological profile and therapeutic potential of BM-573, a combined thromboxane receptor antagonist and synthase inhibitor. Cardiovasc Drug Rev. 2005 Spring;23(1):1-14. [Content Brief]
- [2]. Romero M, et al. Effects of BM-573 on Endothelial Dependent Relaxation and Increased Blood Pressure at Early Stages of Atherosclerosis. PLoS One. 2016 Mar 28;11(3):e0152579. [Content Brief]
Keywords
