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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- CAS No.: 284464-83-1
- Formule: C18H22N4O5S
- Masse moléculaire:406.46
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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TXA2 1.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
0.78 nM
Compound: 1
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Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM
Displacement of [3H]SQ-29548 from TPbeta receptor (long isoform) expressed in COS7 cells at 1 uM
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[PMID: 16759113] |
| COS-7 | IC50 |
1.05 nM
Compound: 1
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Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM
Displacement of [3H]SQ29,548 from TPalpha receptor (short isoform) expressed in COS7 cells at 1 uM
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[PMID: 16759113] |
| HEK293 | IC50 |
0.62 μM
Compound: BM-573
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Antagonist activity at human thromboxane A2 receptor beta over-expressed in HEK293 cells assessed as inhibition of U-46619-induced intracellular calcium mobilization mobilization by fluorescence assay
Antagonist activity at human thromboxane A2 receptor beta over-expressed in HEK293 cells assessed as inhibition of U-46619-induced intracellular calcium mobilization mobilization by fluorescence assay
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[PMID: 23688698] |
| HEK293 | IC50 |
0.7 μM
Compound: BM-573
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Antagonist activity at human thromboxane A2 receptor alpha over-expressed in HEK293 cells assessed as inhibition of U-46619-induced intracellular calcium mobilization by fluorescence assay
Antagonist activity at human thromboxane A2 receptor alpha over-expressed in HEK293 cells assessed as inhibition of U-46619-induced intracellular calcium mobilization by fluorescence assay
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[PMID: 23688698] |
| HEK293 | IC50 |
318.89 nM
Compound: 1
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Activity at TPalpha (short isoform) receptor expressed in HEK293 cells assessed as ability to antagonize U46619-mediated calcium ion mobilization
Activity at TPalpha (short isoform) receptor expressed in HEK293 cells assessed as ability to antagonize U46619-mediated calcium ion mobilization
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[PMID: 16759113] |
| HEK293 | IC50 |
319 nM
Compound: 1, BM-573
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Antagonist activity at human thromboxane A2 receptor isoform alpha expressed in HEK293 cells assessed as inhibition of U46619-induced calcium mobilization
Antagonist activity at human thromboxane A2 receptor isoform alpha expressed in HEK293 cells assessed as inhibition of U46619-induced calcium mobilization
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[PMID: 17630727] |
| HEK293 | IC50 |
53 nM
Compound: 1, BM-573
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Antagonist activity at human thromboxane A2 receptor isoform beta expressed in HEK293 cells assessed as inhibition of U46619-induced calcium mobilization
Antagonist activity at human thromboxane A2 receptor isoform beta expressed in HEK293 cells assessed as inhibition of U46619-induced calcium mobilization
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[PMID: 17630727] |
| HEK293 | IC50 |
53.1 nM
Compound: 1
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Activity at TPbeta (long isoform) receptor expressed in HEK293 cells assessed as ability to antagonize U46619-mediated calcium ion mobilization
Activity at TPbeta (long isoform) receptor expressed in HEK293 cells assessed as ability to antagonize U46619-mediated calcium ion mobilization
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[PMID: 16759113] |
| Platelet | IC50 |
0.509 μM
Compound: BM-573
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Antiplatelet activity against human platelets assessed as inhibition of U-46619-induced platelet aggregation at 1 uM after 1 min
Antiplatelet activity against human platelets assessed as inhibition of U-46619-induced platelet aggregation at 1 uM after 1 min
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[PMID: 23688698] |
Chemical Information
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CAS No. 284464-83-1
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Masse moléculaire 406.46
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Formule C18H22N4O5S
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SMILES
CC(C)(C)NC(NS(C1=C(NC2=CC=C(C)C=C2)C=CC([N+]([O-])=O)=C1)(=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BM-573 Related Classifications
HY-165587 Related Classifications
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