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11

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T1867 Otenaproxesul

ATB 346

Apoptosis; COX Apoptosis; Immunology/Inflammation; Neuroscience
Otenaproxesul (ATB 346) 是一种具有口服活性的非甾体抗炎药,可抑制环氧合酶-1 和 2,具有抗炎生物活性,可用于缓解疼痛的研究。
T36683 Vedaprofen

Quadrisol,PM 150,维达洛芬,CERM 10202

COX; Antibacterial; Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience
Vedaprofen (PM 150) 抑制 COX-1 并通过抗炎活性减少前列腺素 H2 的合成。 Vedaprofen 是一种大肠杆菌滑动钳抑制剂,IC50 为 222 μM,Ki 为 131 μM。
T17191 Bunaprolast

U66858

Lipoxygenase; LTR Immunology/Inflammation; Metabolism
Bunaprolast (U66858) 是一种新型有效的白三烯 B4 (LTB4) 抑制剂。Bunaprolast 具有氧化降解活性,对脂氧合酶 (lipoxygenase)和 TXB2 释放具有抑制作用。
T67959 Pirodomast

Thrombin; Serine Protease Proteases/Proteasome
Pirodomast 是血栓素 A(TXA2)合成酶抑制剂。Pirodomast 能抑制白三烯(LT)D4、C4、E4 的形成和血栓素 B2TXB2)的活性,但对组胺、甲氧胆碱、血清素、LTC4 或血小板活化因子诱导的豚鼠支气管痉挛的拮抗作用较弱或无效。Pirodomast 在体外对豚鼠气管只有微弱的松弛活性。Pirodomast 是一种潜在的抗过敏化合物,在体外可抑制胰蛋白酶的蛋白水解活性,在体内可阻止抗原诱发过敏绵羊的即时和晚期哮喘反应,抑制抗原诱导的过敏绵羊对组胺和卡巴胆碱的气道高反应性。
T10054 CI-949

Others Others
CI-949 is an allergic mediator release inhibitor, which inhibits leukotriene C4/D4 (LTC4/LTD4), histamine, and thromboxane B2 (TXB2) release (IC50s: 0.5 μM, 11.4 μM and 0.1 μM).
T13144 Thiazinamium chloride

Multergan chloride

Others Others
Thiazinamium chloride possesses potent anticholinergic and antiallergic activity and inhibits synthesis of TxB2(IC50 value of 0.2 µM).
T11755 KF 13218

Histone Demethylase Chromatin/Epigenetic
KF 13218 is a selective, potent and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
T36220 2,3-dinor Thromboxane B1

2,3-dinor Thromboxane B1

Thromboxane B2 (TXB2) is released in substantial quantities from aggregating platelets and metabolized during circulation to 11-dehydro TXB2 and 2,3-dinor TXB2. In rats and rabbits, 2,3-dinor TXB1 has been identified as another urinary metabolite of TXB2. However in human urine, only trace amounts of 2,3-dinor TXB1 have been identified. In rats, 2,3-dinor TXB1 is excreted at a much higher rate than 2,3-dinor TXB2 (19.2 ± 4.9 ng/24 hr and 1.6 ± 0.3 ng/24 hr, respectively). Therefore, urinary 2,3-...
T37300 PCTR1

PCTR1

Protectin conjugates in tissue regeneration 1 (PCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid . DHA is oxidized to 16S,17S-epoxy-protectin, which is then converted to PCTR1 by glutathione S-transferase. PCTR1 levels increase during resolution of acute microbial-induced peritonitis in mice. PCTR1 (30 ng, i.p.) administration 12 hours post-infection increases macrophage numbers and activity and shortens the resolution phase of inflammation by 57%. It als...
T83662 2,3-dinor-8-iso Prostaglandin F1α

2,3-dinor-8-iso PGF1α,2,3-dinor-iPF1α-III,2,3-dinor-5,6-dihydro-15-F2t-Isoprostane,2,3-dinor-5,6-dihydro-15-F2t-IsoP

2,3-dinor-8-iso Prostaglandin F1α(2,3-dinor-8-iso PGF1α)是一种异前列腺素和花生四烯酸的活性代谢物,也是血小板聚集抑制剂8-iso PGF2α的产物。它通过花生四烯酸的非酶促自由基过氧化作用形成。2,3-dinor-8-iso PGF1α在孤立的猪视网膜和大脑微血管中引起血管收缩(EC50s分别为12.8和18.5 nM),但在31 µM的浓度下使用时不会引起孤立的大鼠主动脉环的收缩。在1 µM的浓度下使用时,它能增加孤立的猪大脑切片中的血栓素B2TXB2)水平,这一效应可以通过血栓素A合成酶抑制剂CGS 12970、电压门控钙通道抑制剂SKF 96365或烟碱型乙酰胆碱受体(nAChR)拮抗剂α-conotoxin来逆转。
T37507 MCTR3

MCTR3

Maresin conjugates in tissue regeneration 3 (MCTR3) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase, then to MCTR2 by γ-glutamyl transferase, and to MCTR3 by dipeptidase. MCTR3 accelerates tissue regeneration in planaria (1 and 100 nM) approximately as potently as MCTR2 and more potently than MCTR1. Pretreatment with MCTR3 pri...

化合物

Otenaproxesul
Cat.No: T1867
Synonym: ATB 346
Target: Apoptosis, COX
Vedaprofen
Cat.No: T36683
Synonym: Quadrisol,PM 150,维达洛芬,CERM 10202
Target: COX, Antibacterial, Prostaglandin Receptor
Bunaprolast
Cat.No: T17191
Synonym: U66858
Target: Lipoxygenase, LTR
Pirodomast
Cat.No: T67959
Synonym:
Target: Thrombin, Serine Protease
CI-949
Cat.No: T10054
Synonym:
Target: Others
Thiazinamium chloride
Cat.No: T13144
Synonym: Multergan chloride
Target: Others
KF 13218
Cat.No: T11755
Synonym:
Target: Histone Demethylase
2,3-dinor Thromboxane B1
Cat.No: T36220
Synonym: 2,3-dinor Thromboxane B1
Target:
PCTR1
Cat.No: T37300
Synonym: PCTR1
Target:
2,3-dinor-8-iso Prostaglandin F1α
Cat.No: T83662
Synonym: 2,3-dinor-8-iso PGF1α,2,3-dinor-iPF1α-III,2,3-dinor-5,6-dihydro-15-F2t-Isoprostane,2,3-dinor-5,6-dihydro-15-F2t-IsoP
Target:
MCTR3
Cat.No: T37507
Synonym: MCTR3
Target:
Cat. No. Product Name Target Signaling Pathways
T7053 p-Hydroxycinnamic acid

p-Coumaric acid,p-Cumaric acid,p-Hydroxy-cinnamic acid,对羟基肉桂酸,NSC 59260

Thrombin; Endogenous Metabolite; Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation; Metabolism; Proteases/Proteasome
p-Hydroxycinnamic acid (NSC-59260) 是常见的食用酚,可抑制血小板活性,对血栓素 B2 和前列腺素 E2 的 IC50值分别为 371 和 126 μM。
TN5939 Glutinone

赤杨酮,5-Glutinen-3-one

Glutinone (IC50=24 microM) shows a significant effect on thromboxane B2 (TXB2)-release induced by calcium ionophore in human platelets.

天然产物

p-Hydroxycinnamic acid
Cat.No: T7053
Synonym: p-Coumaric acid,p-Cumaric acid,p-Hydroxy-cinnamic acid,对羟基肉桂酸,NSC 59260
Target: Thrombin, Endogenous Metabolite, Prostaglandin Receptor
Glutinone
Cat.No: TN5939
Synonym: 赤杨酮,5-Glutinen-3-one
Target:
TargetMol Loading
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