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23

抑制剂 & 化合物

15

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T60992	COX-1/2-IN-3
	COX-1/2-IN-3 (Compound 7a) 是COX-1和COX-2 的双重抑制剂。COX-2-IN-3 具有低毒性的抗炎活性。
T8656	CAY10404 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T	Apoptosis; Akt; COX	Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Neuroscience; PI3K/Akt/mTOR signaling
	CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) 是一种有效且高度选择性的 COX-2 和 COX-1 抑制剂。它还是 PKB/Akt 和 MAPK 信号通路的有效抑制剂，可诱导 NSC-LC 细胞凋亡，具有镇痛、抗炎和抗癌活性。
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。
T61352	COX-2/5-LOX-IN-3
	COX-2/5-LOX-IN-3 (compound 5b) is a powerful and dual inhibitor of COX-2 and 5-LOX, with IC50 values of 45.73 μM, 5.45 μM, and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. This compound, COX-2/5-LOX-IN-3, shows promise for the investigation of inflammatory diseases [1].
T61760	COX-2-IN-18
	COX-2-IN-18 (Compound 3) is a highly effective COX-2 inhibitor with strong inhibitory activity against COX-2 (IC 50 = 0.775 μM). Its potency is comparable to the reference drug Celecoxib (IC 50 = 0.153 μM). This compound, COX-2-IN-18, shows promise in the field of cancer research [1].
T79361	COX-2/15-LOX-IN-3	Lipoxygenase	Metabolism
	COX-2/15-LOX-IN-3 (compound 5k) 为COX-2/15-LOX的一种双重抑制剂，具有分别为0.075 μM和1.97 μM的IC50值。该化合物能显著抑制LPS诱导的细胞产生促炎细胞因子（IL-6, ROS和NO），表明其具备显著的抗炎活性。
T36457	CAY10416
	Dual cyclooxygenase-2 (COX-2)/5-lipoxygenase (5-LO) inhibitors are potential therapeutic agents for inflammatory diseases and for prostate cancer. CAY10416 is a dual COX-2/5-LO inhibitor with IC50 values of 50 and 3 nM, respectively. The selectivity of CAY10416 for COX is greater than 200-fold for COX-2 versus COX-1. COX-2/5-LO inhibitors such as CAY10416 are also apoptosis-inducing agents and are potentially useful in prostate cancer chemotherapy. In the PC3 human carcinoma cell line, CAY10416 ...
T61606	Indomethacin sodium
	Indomethacin sodium, a powerful and orally active inhibitor of COX1/2, exhibits IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Apart from its potent anti-inflammatory effects, this compound possesses notable anticancer and anti-infective activities. Since it has such versatile attributes, it finds useful applicability in cancer, inflammation, and viral infection research [1] [2] [3].
T71303	Flufenamic Acid-d4
	Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear...
TMIH-0290	Ketorolac-d5-P1
	Ketorolac-d5-P1 是 Ketorolac 的氘代化合物。Ketorolac 的 CAS 号为 74103-06-3。Ketorolac 是非甾体抗炎剂，是非选择性的COX抑制剂，对 COX-1 和 COX-2 的IC50值分别为 20 和 120 nM。
TMIH-0291	Ketorolac-d5-P2
	Ketorolac-d5-P2 是 Ketorolac 的氘代化合物。Ketorolac 的 CAS 号为 74103-06-3。Ketorolac 是非甾体抗炎剂，是非选择性的COX抑制剂，对 COX-1 和 COX-2 的IC50值分别为 20 和 120 nM。
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。
T37919	Prostaglandin F1α PGF1α,Prostaglandin F1α
	Prostaglandin F1α (PGF1α) is the putative metabolite of dihomo-γ-linolenic acid (DGLA) via the cyclooxygenase (COX) pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10-11 M. [1] PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the relative potency of PGF2α. [2] It is only half as active as PGF2α in inducing human respiratory smooth muscle contractions in vitro. [3]
T36221	2-chloro Palmitic Acid
	2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endot...
T36070	(±)5(6)-EET
	5(6)-EET is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5(6)-EET degrades into 5,6-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5(6)-EET has been implicated in the mobilization of calcium and hormone secretion. 5(6)-EET is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhib...
T36418	O-Desmethyl-N-deschlorobenzoyl Indomethacin
	O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin .1It is formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase.2It has also been used in the synthesis of prostaglandin D2receptor antagonists.3 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism ...
T37235	(±)16(17)-EpDPA (±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA
	EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators.[1],[2]Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EET which are prime candidates for the actual active mediator.[3] However, the CYP450 metabolites of eicosapentaenoic acid and docosahex...
T36152	14S(15R)-EET
	14S(15R)-EET is an oxylipin and a cytochrome P450 metabolite of arachidonic acid .114S(15R)-EET binds to isolated guinea pig monocytes with a Kivalue of 612.5 nM in a competitive binding assay using [3H]14(15)-EET.2It induces dilation of precontracted isolated canine epicardial arterioles (EC50= 4 pM) and denuded porcine subepicardial arterioles (EC50= 3 pM).3Unlike 14R(15S)-EET, 14S(15R)-EET does not inhibit COX in enzyme assays or isolated platelets.4 1.Daikh, B.E., Lasker, J.M., Raucy, J.L., ...
T35791	Palmitic acid-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic ...
T35881	Resolvin E2
	Resolvin E2 (RvE2) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acidviaan 18-HEPE intermediate, which is formed by aspirin-acetylated COX-2-mediated oxidation of EPA, by 5-lipoxygenase (5-LO) in human polymorphonuclear (PMN) neutrophils.2,3RvE2 (20 ng/animal) inhibits increases in inflammatory exudate neutrophil infiltration in a mouse model of peritonitis induced by zymosan A .3Hepatic RvE2 levels are increased in m...
T35789	Palmitic acid-1-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 \|1. Santos, M.J., López-Jurado, M., Llopis, J., et a...
T36176	AMK (hydrochloride)
	AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7...
T35597	Neuromedin U-23 (rat) (trifluoroacetate salt)
	Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body ...

化合物

Cat.No: T60992

Cat.No: T8656

Synonym: 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T

Target: Apoptosis, Akt, COX

2,5-dimethyl Celecoxib

Cat.No: T35610

Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor

COX-2/5-LOX-IN-3

Cat.No: T61352

Cat.No: T61760

COX-2/15-LOX-IN-3

Cat.No: T79361

Target: Lipoxygenase

Cat.No: T36457

Indomethacin sodium

Cat.No: T61606

Flufenamic Acid-d4

Cat.No: T71303

Ketorolac-d5-P1

Cat.No: TMIH-0290

Ketorolac-d5-P2

Cat.No: TMIH-0291

Prostaglandin E2 Inhibitor 3

Cat.No: T83773

Synonym: PGE2 Inhibitor 3

Prostaglandin F1α

Cat.No: T37919

Synonym: PGF1α,Prostaglandin F1α

2-chloro Palmitic Acid

Cat.No: T36221

Cat.No: T36070

O-Desmethyl-N-deschlorobenzoyl Indomethacin

Cat.No: T36418

(±)16(17)-EpDPA

Cat.No: T37235

Synonym: (±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA

Cat.No: T36152

Palmitic acid-13C

Cat.No: T35791

Cat.No: T35881

Palmitic acid-1-13C

Cat.No: T35789

AMK (hydrochloride)

Cat.No: T36176

Neuromedin U-23 (rat) (trifluoroacetate salt)

Cat.No: T35597

Cat. No.	Product Name	Target	Signaling Pathways
T6S2023	Harpagoside	Others; COX; NO Synthase	Immunology/Inflammation; Neuroscience; Others
	Harpagoside 是从爪钩草中分离出来的一种天然产物，可抑制COX-1和COX-2活性，并抑制 NO 的产生。
T4S0590	Columbin	Phospholipase; COX; Parasite	Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience
	Columbin 是有口服活性的二萜呋喃内酯，选择性抑制COX-1和COX-2，EC50值为 327 μM 和 53.1 μM，具有抗炎和抗锥虫体作用。
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。
T3S0645	N-trans-Feruloyltyramine Feruloyltyramine,N-Feruloyltyramine,Moupinamide,N-反式阿魏酰酪胺	Others; COX	Immunology/Inflammation; Neuroscience; Others
	N-trans-Feruloyltyramine (Feruloyltyramine) 是从大麻中分离得到的一种生物碱，是COX1和COX2的抑制剂，具有抗氧化和抗炎活性。
T6S1579	Monotropein 水晶兰苷,Monotropeine	Others	Others
	Monotropein (Monotropeine) 是从Morinda officinalis 中获得，能够抑制硫酸葡聚糖硫酸钠诱导的结肠炎小鼠模型中炎性因子的表达。
T4S2126	Ginkgetin 银杏双黄酮,银杏素	Apoptosis; Wnt/beta-catenin; COX; STAT; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; Stem Cells
	Ginkgetin 是从银杏叶中分离得到的一种双黄酮，具有抗肿瘤、抗炎、神经保护、抗真菌的作用。它也是 Wnt 信号抑制剂，IC50值为 5.92 μM。
T4S2326	Cornuside 7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside	ERK; p38 MAPK; NF-κB; JNK	MAPK; NF-κB
	Cornuside (Comuside) 是从山茱萸的果实中分离出的环烯醚萜苷，可用于炎症疾病的研究和促进血液循环。它通过下调 MAPK 和 NF-κB 信号通路抑制肥大细胞介导的过敏反应，用于炎性过敏性疾病中的潜能。
T3S1553	trans-Cinnamaldehyde Cinnamaldehyde,Cinnamic aldehyde,桂皮醛,反式肉桂醛,Cinnamal,Phenylacrolein	COX; Endogenous Metabolite	Immunology/Inflammation; Metabolism; Neuroscience
	trans-Cinnamaldehyde (Phenylacrolein) 是一种能够用于合成反式肉桂醛-β-环糊精复合物，一种能够食用的抗菌涂层，能够延长鲜切水果的保质期。它是一种能够通过烷基异氰化物与乙炔二羧酸二烷基酯的反应来合成高度多官能的呋喃环。
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。
T6S1917	Schisandrol B Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B	P450; Reactive Oxygen Species; Autophagy	Autophagy; Immunology/Inflammation; Metabolism; NF-κB
	Schisandrol B (Besigomsin) 是华中五味子的主要活性成分，具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生，也抑制 P-糖蛋白和CYP3A 的活性。
T6S1572	Sauchinone	ERK; p38 MAPK; NF-κB	MAPK; NF-κB
	Sauchinone 是一种从Saururus chinensis 中获得的非对映异构的木脂素。它通过抑制I-κBα磷酸化和p65核易位来抑制 LPS 诱导的 iNOS，TNF-α 和 COX-2 表达。它具有抗炎和抗氧化活性。
T6S1684	8-Gingerol	Antioxidant; Antibacterial; TRP/TRPV Channel	Membrane transporter/Ion channel; Microbiology/Virology; oxidation-reduction
	8-Gingerol 分离自姜的根状茎，是口服有效的 TRPV1激活剂，EC50值为5.0 µM。8-Gingerol 抑制 COX-2，还能抑制体外 H. pylori 的生长。
T6S1487	Ginsenoside Rg5 人参皂苷Rg5,人参皂甙 Rg5	NF-κB; COX; IGF-1R	Immunology/Inflammation; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors
	Ginsenoside Rg5 是红参的主要成分，可阻断IGF-1与其受体的结合，IC50约为90 nM。它还通过抑制NF-κB p65的 DNA 结合活性来抑制COX-2的 mRNA 表达。它可促进血管生成和改善高血压，具有抗炎和治疗阿尔茨海默病的潜力。
T38330	Collinin
	Collinin is a coumarin that has been found in Z. schinifolium and has diverse biological activities.1,2,3,4 It is active against drug-susceptible and -resistant strains of M. tuberculosis (MIC50s = 3.13-6.25 μg/ml).1 Collinin inhibits LPS-induced nitric oxide (NO) production (IC50 = 5.9 μM) and reduces COX-2 protein levels in RAW 264.7 cells.2 It completely inhibits aggregation of isolated rabbit platelets induced by arachidonic acid , collagen, or platelet activating factor (PAF) when used at a...
T35741	Gliovirin
	Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decrease...

天然产物

Cat.No: T6S2023

Target: Others, COX, NO Synthase

Cat.No: T4S0590

Target: Phospholipase, COX, Parasite

Cat.No: T5S0045

Synonym: 6,8-Dimethoxyumbelliferone,异秦皮啶,Phytodolor,异嗪皮啶

Target: MMP, ERK, p38 MAPK, TLR, COX

N-trans-Feruloyltyramine

Cat.No: T3S0645

Synonym: Feruloyltyramine,N-Feruloyltyramine,Moupinamide,N-反式阿魏酰酪胺

Target: Others, COX

Cat.No: T6S1579

Synonym: 水晶兰苷,Monotropeine

Target: Others

Cat.No: T4S2126

Synonym: 银杏双黄酮,银杏素

Target: Apoptosis, Wnt/beta-catenin, COX, STAT, Autophagy

Cat.No: T4S2326

Synonym: 7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside

Target: ERK, p38 MAPK, NF-κB, JNK

trans-Cinnamaldehyde

Cat.No: T3S1553

Synonym: Cinnamaldehyde,Cinnamic aldehyde,桂皮醛,反式肉桂醛,Cinnamal,Phenylacrolein

Target: COX, Endogenous Metabolite

Cat.No: T3417

Synonym: Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin

Target: Apoptosis, P450, Phospholipase, Reactive Oxygen Species, Opioid Receptor, COX, Antibacterial, RSV, Antifungal

Cat.No: T6S1917

Synonym: Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B

Target: P450, Reactive Oxygen Species, Autophagy

Cat.No: T6S1572

Target: ERK, p38 MAPK, NF-κB

Cat.No: T6S1684

Target: Antioxidant, Antibacterial, TRP/TRPV Channel

Ginsenoside Rg5

Cat.No: T6S1487

Synonym: 人参皂苷Rg5,人参皂甙 Rg5

Target: NF-κB, COX, IGF-1R

Cat.No: T38330

Cat.No: T35741

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