1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. BM-573

BM-573 是一种口服有效的双重血栓素A₂ (TXA₂) 调节剂,其 IC50 为 1.3 nM。BM-573 兼具血栓素合成酶 (TxAS) 抑制和血栓素受体 (TP) 拮抗作用。BM-573 能完全抑制 Arachidonic acid (HY-109590) 或 U-46619 (HY-108566) (TXA₂ 类似物) 诱导的血小板聚集。BM-573 完全阻断人血小板中 TXB₂ (TXA₂ 稳定代谢物) 的生成,且不抑制环氧合酶 (COX-1/COX-2),避免干扰其他前列腺素合成。BM-573 对大鼠胃底平滑肌的 U-46619 诱导收缩有抑制作用 (ED₅₀ = 4.2 μM),但对 PGE₂、PGF₂α、PGI₂ 引起的收缩无影响。BM-573 可用于研究动脉粥样硬化、心肌梗死、肺动脉高压与休克。

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BM-573

BM-573 Chemical Structure

CAS No. : 284464-83-1

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查看 Prostaglandin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

TXA2

1.3 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
COS-7 IC50
0.78 nM
Compound: 1
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
[PMID: 16759113]
COS-7 IC50
1.05 nM
Compound: 1
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
[PMID: 16759113]
HEK293 IC50
0.62 μM
Compound: BM-573
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
[PMID: 23688698]
HEK293 IC50
0.7 μM
Compound: BM-573
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
[PMID: 23688698]
HEK293 IC50
318.89 nM
Compound: 1
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
[PMID: 16759113]
HEK293 IC50
319 nM
Compound: 1, BM-573
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
[PMID: 17630727]
HEK293 IC50
53 nM
Compound: 1, BM-573
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
[PMID: 17630727]
HEK293 IC50
53.1 nM
Compound: 1
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
[PMID: 16759113]
Platelet IC50
0.509 μM
Compound: BM-573
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
[PMID: 23688698]
分子量

406.46

Formula

C18H22N4O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
BM-573
目录号:
HY-165587
需求量: