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28
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T83773 |
Prostaglandin E2 Inhibitor 3
PGE2 Inhibitor 3 |
||
Prostaglandin E2抑制剂3是一种microsomal prostaglandin E合酶-1 (mPGES-1; IC50 = 0.2 µM)的抑制剂,相较于COX-1、COX-2、5-lipoxygenase (5-LO)和soluble epoxide hydrolase (sEH),在10 µM的无细胞试验中表现出对mPGES-1的选择性。在10 µM和1 µM的浓度下,该抑制剂能抑制A549细胞中IL-1β诱导的PGE2生成以及在J774A.1巨噬细胞中,LPS诱导的IL-6和PGE2生成。同时,它还能抑制由钙离子载体A23187单独或结合花生四烯酸和A23187诱导的5-LO产物形成,包括白三烯B4 (LTB4) 和5-H(p)ETE(IC50s分别为4.9和5.2 µM)。在体内,10 mg/kg剂量的Prostaglandin E2抑制剂3能防止在zymosan诱导的小鼠腹膜炎模型中白细胞渗入腹腔液中。 | |||
T78582 |
15-keto-Prostaglandin E2
15-keto-PGE2 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
15-keto-Prostaglandin E2为内源性代谢产物,通过与STAT3Cys259残基结合,抑制STAT3激活作用。该化合物能够结合并稳定EP2与EP4受体,进而抑制乳腺癌细胞生长与进展,并通过激活PPAR-γ促进真菌生长。 | |||
T10046 |
16,16-Dimethyl prostaglandin E2
16,16-dimethyl PGE2 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
16,16-Dimethyl prostaglandin E2 is an orally active vertebrate Hematopoietic stem cells homeostasis critical regulator. It can act through EP2/EP4 and has an interaction with the Wnt pathway. | |||
T63104 | iNOS/PGE2-IN-1 | ||
iNOS/PGE2-IN-1 是一种 iNOS/PGE2 抑制剂,是一种有效的抗炎剂。iNOS/PGE2-IN-1 对 LPS 诱导的 NO 产生表现出抑制作用,具有低致溃疡倾向。 | |||
T83779 |
EP4 Antagonist 14
Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14 |
||
EP4 antagonist 14是一种前列腺素E2(PGE2)受体亚型EP4的拮抗剂,其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募(IC50 = 0.9 nM)。EP4 antagonist 14(10 µM)能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达,这些mRNA编码Il-4、巨噬细胞甘露糖受体1(Mrc1)、几丁质酶样蛋白3(Chil3)、趋化因子(C-X-C)基序配体1(Cxcl1)、表达在髓样细胞上的触发受体2(Trem2)和精氨酸酶-1(Arg1)。在体内,EP4 antagonist 14(每天30 mg/kg),结合抗PD-1抗体,能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。 | |||
T38163 | ML-148 | Dehydrogenase | Metabolism |
ML-148 是 15-羟基前列腺素脱氢酶 (15-PGDH, IC50 = 56 nM) 的特异性抑制剂。 ML-148 可用于分析一组相关的脱氢酶或还原酶以及有关前列腺素信号通路的研究。 | |||
T23861 |
CAY10526
CAY-10526,BTH,CAY 10526 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
CAY10526 (BTH) 是 mPGES-1 的选择性抑制剂,可抑制 NF-κB 信号通路。 | |||
TQ0105 |
CAY10650
|
Phospholipase | Metabolism |
CAY10650 是高效的胞浆磷脂酶A2α抑制剂,IC50=12 nM,能够抑制脂滴形成和 PGE2 分泌。 | |||
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。 | |||
T50005 |
Sertaconazole
|
Antifungal | Microbiology/Virology |
Sertaconazole 是一种广谱抗真菌药。 | |||
T2577 |
Dienogest
地诺孕素,STS 557 |
Apoptosis; Estrogen/progestogen Receptor; Progesterone Receptor; Autophagy | Apoptosis; Autophagy; Endocrinology/Hormones; Others |
Dienogest (STS 557) 是一种孕酮受体激动剂,作用于子宫内膜异位,有口服的子宫内膜活性。 | |||
T1562 |
Rebamipide
Proamipide,OPC12759,瑞巴派特 |
Free radical scavengers; COX; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience; oxidation-reduction |
Rebamipide (OPC12759) 是一种粘膜保护剂,可诱导COX-2表达,增加PGE2水平,并以 COX-2 依赖性方式增强胃粘膜防御。 | |||
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。 | |||
T6665 |
Sertaconazole nitrate
FI-7045,Ginedermofix,FI7056,Ertaczo,硝酸舍他康唑 |
Antibiotic; Antifungal | Microbiology/Virology |
Sertaconazole nitrate (FI-7045) 是一种局部广谱抗真菌药,可用于治疗浅表皮肤和粘膜感染。 | |||
T12352 |
Oxidopamine hydrochloride
6-Hydroxydopamine hydrochloride,6-OHDA hydrochloride,6-羟基多巴胺盐酸盐 |
Mitophagy; Dopamine Receptor; Autophagy | Autophagy; GPCR/G Protein; Neuroscience |
Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) 是一种神经递质多巴胺拮抗剂,可选择性地破坏多巴胺能神经元,是一种广泛使用的神经毒素。 | |||
T12352L |
Oxidopamine hydrobromide
6-Hydroxydopamine hydrobromide,6-羟基多巴胺氢溴酸盐,6-OHDA hydrobromide |
Mitophagy; Dopamine Receptor; Autophagy | Autophagy; GPCR/G Protein; Neuroscience |
Oxidopamine hydrobromide (6-OHDA hydrobromide) 是一种神经递质多巴胺拮抗剂,可选择性地破坏多巴胺能神经元,是一种广泛使用的神经毒素。 | |||
T36619 |
Aligeron
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Aligeron 是一种非选择性的prostaglandin (PG)拮抗剂,对PGF2α和PGE2诱导的猫血压下降有抑制作用,可用于抑制PGF2α诱导的小鼠腹泻和PGE2诱导的大鼠爪水肿。Aligeron 对血管并发症具有抗氧化保护作用。 | |||
TQ0292 |
Grapiprant
AAT-007,RQ-00000007,CJ-023423 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Grapiprant (AAT-007) 是一种选择性EP4 受体拮抗剂,生理配体为前列腺素 E2(PGE2),有用于骨关节炎疼痛和炎症的研究潜力。它取代 [3H]-PGE2(1 nM) 与狗的重组EP4 受体结合,IC50为 35 nM,Ki 为 24 nM。 | |||
T8763 |
PTGR2-IN-1
PTGR2-IN-22 |
Others | Others |
PTGR2-IN-1 是有效的 PTGR2抑制剂,IC50为 ~0.7 μM。它能够提高转染 PTGR2 的 HEK293T 细胞 15-keto-PGE2 依赖的 PPARγ 转录活性。 | |||
T2121 |
SW033291
|
Dehydrogenase | Metabolism |
SW033291 是有效的15-PGDH 抑制剂,与15-PGDH 亲和力高,Ki 为 0.1 nM。它增加骨髓和其他组织中前列腺素 PGE2 的水平。它还可促进组织再生。 | |||
T15681 |
L-161982
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
L-161982 是选择性的 EP4 受体拮抗剂。L-161982 可以抑制 PGE2 诱导的 HCA-7 细胞 ERK 磷酸化和细胞增殖。L-161982 可以缓解胶原诱导的小鼠关节炎。 | |||
T21738 |
PF-9184
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
PF-9184 是一种有效且高度选择性的人微粒体前列腺素 E 合酶 1 (mPGES-1) 的抑制剂,IC50 值为 16.5 nM。PF-9184 体外抑制 IL-1β 诱导的 PGE2 合成。 | |||
T10381 |
AS2717638
|
Others | Others |
AS2717638 是一种具有口服生物活性的,选择性的溶血磷脂酸受体5 (LPA5) 的拮抗剂,其对 hLPA4 的 IC50值为38 nM。AS2717638 还能显著改善 PGE2、PGF2α以及 AMPA 诱导的异位疼痛。 | |||
T15108 |
DG-041
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
DG-041 是高亲和力,选择性的,有效的 EP3受体拮抗剂,在结合和 FLIPR 试验中,IC50分别为 4.6 nM 和 8.1 nM。DG-041通过抑制 PGE2促进血小板聚集。DG-041具有血脑屏障渗透性。 | |||
T3306 |
PF-04418948
PF 04418948,PF04418948 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
PF-04418948 是一种可口服的,选择性的前列腺素EP2受体拮抗剂,IC50为16 nM。 | |||
T67766 |
HHS-0701
|
Others | Others |
HHS-0701,一种硫-三唑交换 (SuTEx) 配体,是酪氨酸反应性前列腺素还原酶 2 (PTGR2) 的有效抑制剂。HHS-0701 可以抑制脂质底物 15-Keto-PGE2 的 PTGR2 代谢。 | |||
T67946 |
EP2 receptor antagonist-2
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
EP2 receptor antagonist-2 (CID891729)为EP2受体拮抗剂,能够抑制PGE2诱导的EP2受体激活,并阻断由N-甲基-D-天冬氨酸(NMDA)引起的乳酸脱氢酶(LDH)释放。 | |||
T23331 |
SC 51089
SC 51089 free base |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
SC 51089 是一种选择性的前列腺素受体 PGE2 拮抗剂,对前列腺素受体亚型具有选择性,具有抗伤害活性,可改善亨廷顿病 R6/1 小鼠模型中的运动缺陷并挽救记忆力下降。 | |||
T15259 |
Evatanepag
CP-533536 free acid,2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Evatanepag (CP-533536 free acid) 是一种 EP2 受体选择性前列腺素 E2 (PGE2) 激动剂,可诱导局部骨形成,EC50 为 0.3 nM。它在大鼠骨折愈合模型中以单剂量局部给药时表现出愈合骨折的能力。 | |||
T14975 |
CJ-42794
CJ-042794 |
Others | Others |
CJ-42794 (CJ-042794)是前列腺素受体 EP4的选择性拮抗剂, 抑制[3H]-PGE2与 EP4受体结合的平均 pKi 为8.5, 对 EP4选择性比 EP1, EP2和 EP3高200多倍。 | |||
T6414 |
Bisacodyl
比沙可啶,Fenilaxan,Dulcolax,Brocalax |
Others | Others |
Bisacodyl (Fenilaxan) 是刺激性缓泻剂,可直接作用于结肠以产生排便。它能够直接激活结肠巨噬细胞来增加 PGE2的分泌。PGE2充当旁分泌因子并减少结肠中 AQP3 的表达,抑制水从腔向血管一侧的转移,进而产生通便作用。 | |||
T28958 |
TG6-129
TG6 129 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
TG6-129 是有效的EP2受体选择性拮抗剂,可降低 butaprost 诱导的 P388D1 巨噬细胞中炎症因子的表达。 | |||
T62061 |
COX-2-IN-6
|
COX; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
COX-2-IN-6 是一种具有有效性、选择性且可口服的环氧化酶-2 (COX-2) 抑制剂,对 COX-2 具有抑制作用,IC50 为 0.84 μM,Ki 为 69 nM。COX-2-IN-6 对 COX-2 驱动的 PGE2 合成具有抑制作用,IC50 为 0.60 μM。COX-2-IN-6 可用于预防结直肠癌。 | |||
T68155 |
Tebufelone
|
Prostaglandin Receptor; LTR | GPCR/G Protein; Immunology/Inflammation |
Tebufelone 是一种体外高效的CO 抑制剂 ,是一种新型的非甾体抗炎药(NSAID),属于二叔丁基苯酚(DTBP)类,在各种动物模型中显示出强大的抗炎、镇痛和抗网膜炎特性。Tebufelone 能有效地抑制前列腺素(PGE2)的形成,阻止大鼠巨噬细胞(IC50 = 20 microM)和人类全血(IC50 = 22 microM)中脂氧酶途径的产物[白三烯(LTB4)]的体外形成。 | |||
T12103 |
MR-L2
|
PDE | Metabolism |
MR-L2 是可逆的、非竞争性的长型异构体磷酸二酯酶 -4激活剂,可以激活代表性的 PDE4 长型异构体 (PDE4A4、PDE4B1、PDE4C3、PDE4D5)。它可抑制 PGE2- 诱导的 MDCK 细胞囊肿形成,其EC50=1.2 µM。 | |||
T35610 |
2,5-dimethyl Celecoxib
|
Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells |
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。 | |||
T36728 |
9-deoxy-9-methylene Prostaglandin E2
9-deoxy-9-methylene Prostaglandin E2 |
||
9-deoxy-9-methylene Prostaglandin E2 (9-deoxy-9-methylene PGE2) is a stable, isosteric analog of PGE2 . 9-deoxy-9-methylene PGE2 retains the biological profile of PGE2 with fewer side effects. In the rat 9-deoxy-9-methylene PGE2 is equipotent to PGE2 in decreasing blood pressure. It also stimulates the gerbil colon and primate uterus at the same potency as PGE2. | |||
T35991 |
ent-Prostaglandin E2
ent-Prostaglandin E2 |
||
Enzymatically-derived prostaglandin E2 (PGE2) is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings of oxidative stress via the isoprostane pathway. A proposed mechanism for the formation of rac-PGE2 involves the base catalyzed equilibration from 15-E2t-isoprostane (8-iso-PGE2), g... | |||
T26497 |
AAT-008
AAT008 |
||
AAT-008 is a PGE2 receptor EP4 antagonist. | |||
T38342 |
11-deoxy Prostaglandin E2
11-deoxy Prostaglandin E2 |
||
11-deoxy Prostaglandin E2 (11-deoxy PGE2) is a stable, synthetic analog of PGE2 . In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and contracts human respiratory tract smooth muscle with potencies ranging from 5 to 30 times higher than PGF2α . | |||
T37839 |
20-hydroxy Prostaglandin E2
20-hydroxy Prostaglandin E2 |
||
20-hydroxy Prostaglandin E2 (20-hydroxy PGE2) is a product of cytochrome P450 metabolism of PGE2 . ω-Oxidation at C-20 followed by β-oxidation and the loss of up to four carbons from the lower side chain is a prominent metabolic pathway for PGE2. 20-hydroxy PGE2 is the putative first intermediate in this chain of chemical transformations. | |||
T36144 |
11β-Prostaglandin E2
11β-PGE2,11β-Prostaglandin E2 |
||
11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM.[1] 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2.2 11β-PGE2 inhibits PGE2 binding to the prostaglandin transporter protein with a Ki of 56 nM.[3] . | |||
T36168 |
8-iso-16-cyclohexyl-tetranor Prostaglandin E2
8-iso-16-cyclohexyl-tetranor Prostaglandin E2 |
||
8-iso Prostaglandin E2 (8-iso PGE2) is one of several isoprostanes produced from polyunsaturated fatty acids during lipid peroxidation. 8-iso-16-cyclohexyl-tetranor PGE2 is a synthetic analog of 8-iso PGE2. There are no published studies on the pharmacological properties of 8-iso-16-cyclohexyl-tetranor PGE2. | |||
T36154 |
15(S)-15-methyl Prostaglandin E2
15(S)-15-methyl Prostaglandin E2 |
||
15(S)-15-methyl PGE2 is a potent, metabolically stable analog of PGE2. It is a potent gastric antisecretory and antiulcer compound. 15(S)-15-methyl PGE2 binds to human myometrium with twice the affinity of PGE2 and is ten times more potent than PGE1 in contracting uterine smooth muscle. | |||
T38305 |
tetranor-PGAM
|
||
Prostaglandin E2 (PGE2), one of the most widely investigated PGs, can be used as a biomarker of inflammation, disease state, or therapeutic effectiveness. However due to its rapid metabolism, direct measurement of PGE2 in biological samples is difficult. The major urinary metabolite of PGE2, tetranor-PGEM, serves as an indirect marker of PGE2 biosynthesis. Though like PGE2, tetranor-PGEM is also chemically unstable. tetranor-PGAM is a dehydration product of tetranor-PGEM and can be measured as a... | |||
T27981 |
MB-28767
M&B 28767,MB28767 |
||
MB-28767 is an agonist of prostaglandin E2 (PGE2) receptor. | |||
T71594 | SC 42867 | ||
SC 42867 is a PGE2 antagonist. | |||
T11792 | KW-8232 free base | Others | Others |
KW-8232 free base can reduces the biosynthesis of PGE2, is an anti-osteoporotic agent. | |||
T27243 |
Efipladib
PLA-902,PLA 902,PLA902 |
||
Efipladib is a phospholipase inhibitor. Efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid. | |||
T37773 |
tetranor-PGEM
tetranor-Prostaglandin E Metabolite,tetranor-PGEM |
||
tetranor-PGEM is the major urinary metabolite of PGE1 and PGE2, and is used as a marker of PGE2 biosynthesis.[1],[2] About 15% of an infused dose of PGE2 appears as this metabolite in the urine of humans. Normal healthy males excrete 7-40 μg of tetranor-PGEM over a 24-hour period.[1] |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5014 |
Prostaglandin E2
地诺前列酮,前列腺素 E2,PGE2,Dinoprostone,Prostaglandin E2 (PGE2) |
Endogenous Metabolite; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism |
Prostaglandin E2 (PGE2) 是一种天然激素,参与人体内的各种生理过程,包括平滑肌收缩和放松、调节血管扩张和收缩、调节血压和炎症调节。 | |||
T5758 |
sphondin
6-甲氧基当归素,牛防风素,牛防风素 |
COX; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Sphondin 具有抗惊厥、抗炎和抗增殖活性,对 IL-1beta 诱导的 A549 细胞中 COX-2 蛋白水平和 PGE(2) 释放的增加具有抑制作用。 | |||
T5774 |
Demethylsuberosin
7-去甲基软木花椒素,7-demethylsuberosin |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
7-Demethylsuberosin (7-demethylsuberosin) 是一种分离自 Angelica gigasNakai 中的香豆素类化合物,具有抗炎作用。 | |||
T5727 |
CAFESTOL
咖啡醇,咖啡油醇 |
ERK; NF-κB; COX; PGE Synthase | Immunology/Inflammation; MAPK; Neuroscience; NF-κB |
Cafestol 是咖啡特有的一种二萜,可靶向 AP-1 抑制ERK,有化学预防、抗肿瘤、保肝、抗氧化和抗炎作用。它通过抑制NF-kB 活化途径强烈的抑制 PGE2的产生,还抑制 LGE 激活的 RAW264.7 细胞中的PGE2产生和环氧合酶(COX-2)的 mRNA 表达。 | |||
T6S0840 |
Engeletin
Dihydrokaempferol 3-rhamnoside,黄杞苷 |
NF-κB; Reductase | Endocrinology/Hormones; Metabolism; NF-κB |
Engeletin (Dihydrokaempferol 3-rhamnoside) 是一种黄酮苷类物质,从hymenaea martiana 中获得,抑制NF-κB 信号通路的激活,具有抗炎、缓解疼痛、消肿、利尿、抗菌等作用。 | |||
TN2091 |
Polygalacin D
|
Apoptosis; IAP | Apoptosis |
Polygalacin D 是从桔梗中分离的一种天然产物,具有抗癌和抗增殖特性。它通过 PI3K/Akt 途径诱导凋亡。它抑制 IAP 蛋白家族的表达,并通过抑制 GSK3β,Akt 的磷酸化和 PI3K 的表达来阻断 PI3K/Akt 途径。 | |||
T2791 |
Pectolinarin
柳穿鱼叶苷,大蓟苷 |
Apoptosis; Others; NO Synthase; Prostaglandin Receptor; Interleukin | Apoptosis; GPCR/G Protein; Immunology/Inflammation; Others |
Pectolinarin 抑制 IL-6和 IL-8分泌以及 PGE2和 NO 产生,可通过抑制 PI3K/Akt 途径来抑制细胞增殖和炎症反应并诱导凋亡,具有抗炎活性。 | |||
T6S0077 |
Byakangelicol
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COX | Immunology/Inflammation; Neuroscience |
Byakangelicol 是一种分离自白芷的白三醇,能够抑制环加氧酶-2的表达及活性,从而减少白细胞介素-1β诱导的 A549 细胞中前列腺素 E2 的释放。它可用于研究气道炎症。 | |||
T5S1981 |
alpha-Cyperone
(+)-α-Cyperone,α-香附酮,α-Cyperone |
Others; Endogenous Metabolite | Metabolism; Others |
alpha-Cyperone (α-Cyperone) 与 IL-6, Cox-2, Cdc42, Nck-2, Rac1 的表达下调相关,从而能够抑制炎症反应。 | |||
T4S0867 |
Pogostone
DHELWANGIN,广藿香酮 |
Apoptosis; Antibacterial; Autophagy | Apoptosis; Autophagy; Microbiology/Virology |
Pogostone (DHELWANGIN) 是从薄荷中分离出,对革兰氏阴性菌、革兰氏阳性菌、大肠埃希菌等具有强效抗菌、抗真菌活性。它诱导细胞凋亡和自噬。 | |||
T3926 |
Echinatin
刺甘草查尔酮,Retrochalcone |
Free radical scavengers | oxidation-reduction |
Echinatin (Retrochalcone) 是分离自中草药甘草中,具有保肝和抗炎活性。在大鼠中,它可以被快速吸收和消除,并广泛分布,绝对生物利用度约为 6.81%。 | |||
TQ0169 |
Inulicin
1-O-Acetylbritannilactone,旋覆花内酯 |
FAK; NF-κB; COX; Src | Angiogenesis; Cytoskeletal Signaling; Immunology/Inflammation; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors |
Inulicin (1-O-Acetylbritannilactone) 是从欧亚旋覆花中提取的一种天然产物,可抑制 VEGF 介导的Src 和FAK 活化,抑制NF-κB 活化和易位,以及抑制 LPS 诱导的PGE2产生和COX-2表达。 | |||
T5S0045 |
Isofraxidin
6,8-Dimethoxyumbelliferone,异秦皮啶,Phytodolor,异嗪皮啶 |
MMP; ERK; p38 MAPK; TLR; COX | Immunology/Inflammation; MAPK; Neuroscience; Proteases/Proteasome |
Isofraxidin (Phytodolor) 是来自刺五加的香豆素成分,抑制MMP-7表达和人肝癌细胞侵袭。它作用于肝癌细胞,抑制ERK1/2磷酸化。它减弱iNOS 和COX-2表达,还抑制TLR4/髓样分化蛋白 2 复合物的形成。 | |||
T3417 |
Amentoflavone
Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin |
Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal | Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB |
Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物,有抗炎、抗氧化和神经保护等作用。 | |||
T2S2335 |
Dehydroevodiamine
DHED,去氢吴茱萸碱 |
Others; NF-κB; COX; PGE Synthase; NO Synthase | Immunology/Inflammation; Neuroscience; NF-κB; Others |
Dehydroevodiamine (DHED) 是从吴茱萸中分离出的一种喹唑啉生物碱,可抑制 LPS 诱导的小鼠巨噬细胞中iNOS、COX-2、PGE2和NF-κB 的表达,对豚鼠心室肌细胞具有抗心律失常作用。 | |||
T3744 |
Veratric acid
Veratrumenoic acid,藜芦酸,3,4-Dimethoxybenzoic acid |
Reactive Oxygen Species; COX | Immunology/Inflammation; Metabolism; Neuroscience; NF-κB |
Veratric acid (3,4-Dimethoxybenzoic acid) 是从蔬菜和水果中得到的一种可口服多酚,具有抗氧化、保护心血管和抗炎活性。当细胞受到 UVB 辐射时,它能够减少上调的 COX-2 表达,降低 PGE2 和 IL-6 水平。 | |||
T6S0735 |
Flavokawain B
黄卡瓦胡椒素B,Flavokavain B,Flavokawin B,2'-Hydroxy-4',6'-Dimethoxychalcone |
Apoptosis; Others | Apoptosis; Others |
Flavokawain B (Flavokavain B) 是从卡瓦醉椒的根提取物中,分离出的查尔酮。它是一种凋亡诱导剂,可抑制各种癌细胞株生长。它以极低的无毒浓度抑制人脑内皮细胞的迁移和血管形成,具有抗血管生成活性。 | |||
T3868 |
Agnuside
牡荆油,穗花牡荆苷,chasteberry oil |
COX; Prostaglandin Receptor; P-gp | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience |
Agnuside (chasteberry oil) 是从黄荆中分离得到的一种天然产物,可下调炎性介质PGE2和LTB4,减少细胞因子的表达,具有抗关节炎活性。 | |||
T3S0153 |
Xanthatin
苍耳亭,叶黄制菌素 |
Apoptosis; VEGFR; Lipoxygenase; Wnt/beta-catenin; Antibacterial | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Metabolism; Microbiology/Virology; Stem Cells; Tyrosine Kinase/Adaptors |
Xanthatin 是一种从Xanthium strumarium 叶子中提取的天然产物,可诱导细胞凋亡。它抑制布鲁氏菌的IC50值为 2.63 μg/ mL,对寄生虫特异性锥虫硫磷还原酶具有不可逆的弱抑制作用。它通过抑制PGE2的合成和 5-脂氧合酶的活性而显示出抗炎活性。 | |||
T2S0765 |
Epibetulinic acid
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NO Synthase; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Epibetulinic acid 对细菌内毒素刺激的小鼠巨噬细胞 (RAW 264.7) 中 NO 和前列腺素 E(2) 的产生具有有效的抑制作用,IC50分别为 0.7 和 0.6 μM,具有抗炎活性。 | |||
TN1871 |
Ligustroside
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EGFR; Lipoxygenase; COX | Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; Metabolism; Neuroscience; Tyrosine Kinase/Adaptors |
Ligustroside shows little antioxidant, and anti-inflammatory properties, it shows a significant inhibition effect on prostaglandin E2 (PGE2)-release. Ligustroside shows moderate antiviral activities against parainfluenza type 3 virus. | |||
T38635 |
Kdo2-Lipid A ammonium
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TNF; TLR; Prostaglandin Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation |
Kdo2-Lipid A ammonium (KLA) 是一种具有选择性和有效性的 TLR4 激动剂,属于一种脂多糖。Kdo2-Lipid A ammonium 促使 TNF 和 PGE2 的释放。 | |||
TN4465 |
Luvangetin
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COX; Prostaglandin Receptor; Antifection | GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience |
Luvangetin may have anti-inflammatory activity, it can inhibit NO and PGE2 production in LPS-stimulated BV2 cells. Luvangetin shows significant protection against pylorus-ligated and aspirin-induced gastric ulcers in rats and cold restraint stress-induced | |||
TN2169 |
Saikogenin D
柴胡皂甙元 D,皂苷元 D |
IL Receptor; Calcium Channel; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism |
Saikogenin D possesses a dual effect: an inhibition of A23187-induced PGE2 production without a direct inhibition of cyclooxygenase activity; and an elevation of [Ca2+]i that is attributed to Ca2+ release from intracellular stores. Saikogenin D has immuno | |||
T37774 |
Thielavin A
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Thielavin A is a fungal metabolite originally isolated from T. terricola that is related to thielavin B . Thielavin A inhibits COX, blocking both the conversion of arachidonic acid to prostaglandin H2 and the conversion of PGH2 to PGE2 . Thielavin A also inhibits glucose-6-phosphatase in rat liver microsomes (IC50 = 4.6 μM). It is a non-competitive inhibitor of α-glucosidase from S. cerevisiae (IC50 = 23.8 μM; Ki = 27.8 μM). | |||
TN4489 | Manassantin A | ERK; cAMP; TNF; NF-κB; MAPK; COX; HIF; Prostaglandin Receptor; JNK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; MAPK; Neuroscience; NF-κB; Stem Cells |
Manassantin A is a high potent HIF-1 inhibitor, it protects the gastric mucosa from ethanol-induced acute gastric injury, and suggest that these protective effects might be associated with COX/PGE2 stimulation, inhibition of iNOS production and NF-κB act | |||
TN4879 | Questinol | IL Receptor; TNF; COX; Prostaglandin Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Questinol exhibits significant anti-obesity activity. It shows anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, it can inhibit the production of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6 and inhibit NO an | |||
TN4046 | Excisanin A | MMP; FAK; PARP; GSK-3; NF-κB; Wnt/beta-catenin; Akt; Caspase; PI3K; Prostaglandin Receptor; JNK | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; MAPK; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors |
ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the ... |