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7

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T17189 U-46619

9,11-Methanoepoxy PGH2

Progesterone Receptor; PPAR DNA Damage/DNA Repair; Metabolism; Others
U-46619是一种有效的TXA2激动剂,是一种血栓素A2类似物(内过氧化物),有诱导肌球蛋白轻链9 (Myl9)基因缺失小鼠主动脉平滑肌(SM)收缩的功能。
T6594 MNS

Syk; Src; p97 Angiogenesis; Tyrosine Kinase/Adaptors; Ubiquitination
MNS 是一种酪氨酸激酶抑制剂和广谱抗血小板药物,是一种 β-硝基苯乙烯衍生物。它完全抑制 U46619 (IC50:2.1 μM)、ADP (IC50:4.1 μM)、花生四烯酸 (IC50:5.8 μM)、胶原 (IC50:7.0 μM)和凝血酶 (IC50:12.7 μM)诱导的血小板聚集,并抑制 Src (IC50:27.3 μM)、Syk (IC50:2.8 μM) 和 FAK (IC50:97.6 μM)。
T72591 Sp-5,6-DCl-cBIMPS

Sp-5,6-DCl-cBIMPS 为一种高效特异的 cAMP 依赖性蛋白激酶(cAMP-PK)激活剂,能够促进胰岛素释放,并抑制U46619引起的血小板Rho、Gq及G12/G13的激活[3]。
T35506 (±)12-HEPE

(±)12-HEPE is produced by non-enzymatic oxidation of EPA. It contains equal amounts of 12(S)-HEPE and 12(R)-HEPE. The biological activity of (±)12-HEPE is likely mediated by one of the individual isomers, most commonly the 12(S) isomer in mammalian systems. 12-HEPE inhibits platelet aggregation with the same potency as 12-HETE, exhibiting IC50 values of 24 and 25 &#181M, respectively. [1] These compounds are also equipotent as inhibitors of U46619-induced contraction of rat aorta (IC50s = 8.6-8....
T36150 14,15-EE-5(Z)-E

Epoxyeicosatrienoic acids (EETs), such as 11(12)-EET and 14(15)-EET, are cytochrome P450 metabolites of arachidonic acid that have been identified as endothelium-derived hyperpolarizing factors with vasodilator activity. 14,15-EE-5(Z)-E is a structural analog of 14,15-epoxyeicosatrienoic acids (14,15-EET) that antagonizes EET-induced relaxation of vascular smooth muscle. Relaxation of U46619-constricted bovine arteries by 14,15-EET could be inhibited approximately 80% by 14,15-EE-5(Z)-E at a con...
T36550 CAY10535

TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for ...
T36717 RWJ-56110 dihydrochloride

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell ap...

化合物

U-46619
Cat.No: T17189
Synonym: 9,11-Methanoepoxy PGH2
Target: Progesterone Receptor, PPAR
MNS
Cat.No: T6594
Synonym:
Target: Syk, Src, p97
Sp-5,6-DCl-cBIMPS
Cat.No: T72591
Synonym:
Target:
(±)12-HEPE
Cat.No: T35506
Synonym:
Target:
14,15-EE-5(Z)-E
Cat.No: T36150
Synonym:
Target:
CAY10535
Cat.No: T36550
Synonym:
Target:
RWJ-56110 dihydrochloride
Cat.No: T36717
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN6975 Cirsiumaldehyde

5,5’-oxydimethylenebis(2-furfural)

Platelet aggregation Others
Cirsiumaldehyde 是一种从Lobelia chinensis、Cornus officinalis 成熟果实和 Hippophae rhamnoides 果实中分分离出的化合物。Cirsiumaldehyde 在胶原蛋白存在下对 U46619 诱导(1~5 uM)的大鼠血小板聚集的抑制浓度为 0.8~1.0 ug/mL。
TN5569 2-Deacetoxytaxinine B

2-Deacetoxytaxinine B is a strongly inhibitor against U46619-induced aggregation, it shows strong inhibitory effects against arachidonic acid (AA)-induced aggregation.

天然产物

Cirsiumaldehyde
Cat.No: TN6975
Synonym: 5,5’-oxydimethylenebis(2-furfural)
Target: Platelet aggregation
2-Deacetoxytaxinine B
Cat.No: TN5569
Synonym:
Target:
TargetMol Loading
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