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41

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7739	L-Leucyl-L-Leucine methyl ester hydrochloride Leu-Leu-ome hydrochloride	Others; Endogenous Metabolite	Metabolism; Others
	L-Leucyl-L-Leucine methyl ester hydrochloride (Leu-Leu-ome hydrochloride) 是一种人单核细胞或多形核白细胞产生的 L-亮氨酸甲酯的二肽缩合产物，能够选择性消除具有细胞毒性潜能的淋巴细胞，也能够诱导溶酶体途径应激。
T27026	CJ-13,610 CJ 13610,CJ-13610	Lipoxygenase	Metabolism
	CJ-13,610 是一种具有口服活性的非氧化还原型 5-脂氧合酶 (5-LOX) 抑制剂。 CJ-13,610 抑制白三烯 B4 的生物合成并调节巨噬细胞中 IL-6 mRNA 的表达。
T68166	Traxanox	Others	Others
	Traxanox 是一种可口服的利尿剂。Traxanox 在体外增强小鼠腹膜巨噬细胞或大鼠腹膜多形核白细胞对酵母颗粒的吞噬作用。Traxanox 对抑制BALB/c小鼠抗体产生的恢复作用。
T22946	LY255283 LY 255283	Leukotriene Receptor	GPCR/G Protein
	LY255283 是白三烯 B4 (LTB4) 受体的特异性拮抗剂，抑制人外周血多形核白细胞和由钙离子载体 A23187 激活的单核细胞中 LTB(4) 的产生。
T36879L	H-Leu-Leu-OMe . HBr H-Leu-Leu-OMe . HBr (16689-14-8 Free base)	Others	Others
	H-Leu-Leu-OMe . HBr 是由人单核细胞或多形核白细胞产生的L-亮氨酸甲酯的二肽缩合产物。 H-Leu-Leu-OMe . HBr 诱导内溶酶体途径应激并选择性地消除具有细胞毒性潜力的淋巴细胞。
T68166L	Traxanox TFA Traxanox TFA(58712-69-9 Free base)	Others	Others
	Traxanox TFA 是一种可口服的利尿剂。Traxanox TFA 在体外增强小鼠腹膜巨噬细胞或大鼠腹膜多形核白细胞对酵母颗粒的吞噬作用。Traxanox TFA 对抑制BALB/c小鼠抗体产生的恢复作用。
T69110	Aseanostatin P5
	Aseanostatin P5 inhibits myeloperoxidase (MPO) release from human polymorphonuclear leukocytes.
T24305	L 651142 L651,142,L651142,L-651,142,L 651,142,L-651142
	L 651142 is a weak inhibitor of the platelet-activating factor receptor. It is also binding to polymorphonuclear leukocytes.
T24328	L 680833 L680,833,L680833,L-680,833,L 680,833,L-680833
	L 680833 is an orally active monocyclic beta-lactam human polymorphonuclear leukocyte elastase inhibitor.
T22526	BML-111 5(S),6(R)-7-trihydroxymethyl Heptanoate	Others	Others
	inhibits leukotriene B4 (LTB4)-induced polymorphonuclear neutrophils (PMN) chemotaxis
T71025	KP 10614
	KP 10614 is a new prostacyclin analog that inhibits platelet-polymorphonuclear leukocyte interaction.
T27408	Gea 3162 Gea3162,Gea-3162
	Gea 3162 is a potent inhibitor of ADP-induced platelet aggregation in platelet rich plasma (PRP). GEA 3162 stimulates cGMP production in granulocytes, platelets, and polymorphonuclear leukocytes.
T0260L	Meclofenamate sodium hydrate INF 4668,CI583,CI-583,INF-4668,CI 583,INF4668
	Meclofenamate sodium is a potent non-steroidal anti-inflammatory agent, which can specifically inhibit chemokine-induced human polymorphonuclear leukocyte function: chemotaxis, degranulation, and superoxide anion free radical production.
TP2395	Nph-peptide
	Nph-peptide can be used for photoaffinity labeling of the N-formyl peptide receptor site of intact human polymorphonuclear leukocytes.
T15825	LY 178002	Retinoid Receptor	Metabolism
	LY 178002 is an effective inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2 (IC50: 0.6 μM for 5-lipoxygenase). LY 178002 also inhibits cellular production of LTB4 by human polymorphonuclear leukocytes and displays relatively weak inhibition on cycloox
T37460	Lipoxin B4 Lipoxin B4
	Lipoxin B4 (LXB4) is a positional isomer of LXA4 produced by the metabolism of 15-HETE or 15(S)-HpETE by human leukocytes. At a concentration of 100 nM, LXB4 inhibits polymorphonuclear leukocyte (PMN) migration stimulated by leukotriene B4 and inhibits LTB4-induced adhesion of PMNs with an IC50 value of 0.3 nM.
T38308	Lipoxin B4 methyl ester
	Lipoxin B4 (LXB4) methyl ester is a lipid soluble prodrug form of the transcellular metabolite LXB4 . LXB4 is a positional isomer of LXA4 produced by the metabolism of 15-HETE or 15-HpETE by human leukocytes. At a concentration of 100 nM, LXB4 inhibits polymorphonuclear leukocyte (PMN) migration stimulated by leukotriene B4 and inhibits LTB4-induced adhesion of PMNs with an IC50 value of 0.3 nM.
T21962	HZ52
	HZ52 是一种有效可逆的5-脂氧合酶(5-LO)抑制剂，在完整的人类多形核白细胞中可阻断白三烯的合成，IC50为 0.7 μM。
T36043	17(R)-Protectin D1 17(R)-Protectin D1
	17(R)-Protectin D1 is an aspirin-triggered epimer of the specialized pro-resolving mediator protectin D1 .1It decreases leukotriene B4-induced transendothelial migration of human polymorphonuclear (PMN) neutrophils when used at concentrations ranging from 0.1 to 10 nM. 17(R)-Protectin D1 (0.01-10 ng) reduces the recruitment of neutrophils in a mouse model of TNF-α-induced peritonitis. 1.Serhan, C.N., Fredman, G., Yang, R., et al.Novel proresolving aspirin-triggered DHA pathwayChem. Biol.18(18)97...
T74650	JPE-1375
	JPE-1375 是一种补体C5a 受体 1 (C5aR1) 拮抗剂。JPE-1375 能有效抑制小鼠体内多形核白细胞动员 (EC50=6.9 µM) 和降低TNF 水平 (EC50=4.5 µM)。JPE-1375 可用于自身免疫性和炎性疾病的研究。
T37382	1,2,3-Trieicosapentaenoyl-rac-glycerol
	1,2,3-Trieicosapentaenoyl-rac-glycerol (EPA-TG) is a glycerol ester of eicosapentaenoic acid , which is an ω-3 fatty acid. An EPA-TG emulsion, administered i.v., lowers leukotriene B4 production by 40% in polymorphonuclear leukocytes from rabbits and reduces platelet aggregation. It suppresses natural killer cell activity both in vitro and in vivo, in human lymphocytes and murine spleens, respectively, with the in vivo effects lasting up to seven days.
T37168	Resolvin D1 methyl ester Resolvin D1 methyl ester
	Resolvin D1 is produced physiologically from the sequential oxygenation of docosahexaenoic acid by 15- and 5-lipoxygenase . It reduces human polymorphonuclear leukocyte transendothelial migration, the earliest event in acute inflammation, with an EC50 value of ~30 nM. RvD1 methyl ester is a methyl ester version of the free acid that may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracell...
T37975	13(S)-HODE-biotin
	13(S)-HODE is the lipoxygenase metabolite of linoleic acid. 13(S)-HODE modulates the platelet-activating factor, leukotriene B4, and formyl-Met-Leu-Phe-induced calcium influx in human polymorphonuclear leukocytes. The mechanism by which 13(S)-HODE elicits its inhibitory effect is still unclear. The use of biotinylated 15(S)-HETE as a probe for detecting binding proteins and/or receptors that specifically bind 15(S)-HETE provides a basis for similar use of 13(S)-HODE-biotin.
T38363	MeOSuc-AAPV-pNA
	Proteinase 3 (PR3, myeloblastin) is a polymorphonuclear leukocyte serine proteinase that degrades matrix proteins including fibronectin, laminin, vitronectin, and collagen type IV to generate antimicrobial peptides. Neutrophil elastase is a serine proteinase that is secreted by neutrophils during inflammation to destroy pathogens. Evaluating these enzymes is helpful to understanding inflammatory autoimmune processes. MeOSuc-AAPV-pNA is a highly sensitive peptide substrate that is hydrolyzed by b...
T37649	5(S),12(S)-DiHETE
	5(S),12(S)-DiHETE is a natural bioactive lipid derived from arachidonic acid . It is synthesized by glycogen-induced rabbit peritoneal polymorphonuclear leukocytes (PMNLs) incubated with AA. 5(S),12(S)-DiHETE can be produced by successive oxygenation of AA by 5-lipoxygenase (5-LO) in platelets and 12-LO in leukocytes. It can also be synthesized from 12(S)-HETE by 5-LO, in the presence of 5-LO activating protein (FLAP), activated with calcium ionophore. 5(S),12(S)-DiHETE is an epimer of leukotrie...
T34917	Traxanox sodium Y 12141,Y12141,Y-12141
	Traxanox sodium 是一种可口服的利尿剂。Traxanox sodium 在体外增强小鼠腹膜巨噬细胞或大鼠腹膜多形核白细胞对酵母颗粒的吞噬作用。Traxanox sodium 对抑制BALB/c小鼠抗体产生的恢复作用。
T37260	14,15-dehydro Leukotriene B4 14,15-dehydro Leukotriene B4
	Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from arachidonic acid through the 5-lipoxygenase pathway. It promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, enhancement of lysosomal enzyme release, superoxide anion production, chemotaxis, and chemokinesis. At least two LTB4 receptors, termed BLT1 and BLT2, have been identified. 14,15-dehydro LTB4 is a LTB4 receptor antagonist that has a higher binding affinity for BLT1, demonstrating a Ki value ...
T36671	C2 Phytoceramide (t18:0/2:0)
	C2 Phytoceramide is a bioactive semisynthetic sphingolipid that inhibits formyl peptide-induced oxidant release (IC50 = 0.38 μM) in suspended polymorphonuclear cells. It increases COX-2 protein levels 15-fold through ERK signaling. It induces death of keratinocytes (20% viability) with an ED50 value of 30 μM, the same concentration at which 35% of cells in a TUNEL assay are apoptotic. C2 Phytoceramide also has antiproliferative effects in CHO cells, with greater than 80% cytotoxicity achieved at...
T37259	14(S)-HDHA
	Docosahexaenoic acid is a nutritionally-derived ω-3 fatty acid that is abundant in the brain and the retina and is thought to be important in early development and for therapeutic approaches to inflammatory disorders and cancer. 14(S)-HDHA is an oxygenation product of DHA that serves as a precursor to maresin 1 , an anti-inflammatory, pro-resolving mediator that prevents polymorphonuclear neutrophil (PMN) infiltration and stimulates macrophage phagocytosis. At doses as low as 0.2 ng/mouse 14(S)-...
T38103	Defensin HNP-3 (human) (trifluoroacetate salt)
	Defensin HNP-3 is a peptide secreted by human polymorphonuclear leukocytes (PMNs) that has antimicrobial properties. It induces lysis of mammalian cells when used at a concentration of 25 μg/mL. It also inhibits growth of E. faecalis (ED50 = 100 nM) and clinical isolates of P. aeruginosa (MIC90 = 4 μM). HNP-3 binds to recombinant HIV-1 envelope glycoprotein (gp120) and human CD4 (Kds = 52.8 and 34.9 nM, respectively). It also binds to recombinant, immobilized human surfactant protein D (SP-D; Kd...
TP1354	ATI-2341 TFA (1337878-62-2 free base) ATI-2341 TFA
	ATI-2341 is an effective functionally selective allosteric agonist for the c-x-c chemokine receptor type 4 (CXCR4), which ACTS as a biased ligand in favor of G G G G G 1 activation instead of G G G G G 13.ATI-2341 activates the inhibitory heterotrimer G p
T37265	15(R)-Lipoxin A4 15(R)-Lipoxin A4,AT-Lipoxin A4
	Lipid-derived lipoxins are produced at the site of vascular and mucosal inflammation where they down-regulate polymorphonuclear leukocyte recruitment and function. 15(R)-Lipoxin A4 (15(R)-LXA4) is derived from the aspirin-triggered formation of 15(R)-HETE from arachidonic acid. [1] [2] 15(R)-LXA4 inhibits LTB4-induced chemotaxis, adherence, and transmigration of neutrophils with twice the potency of LXA4 demonstrating activity in the nM range.[2] [3] The anti-inflammatory effects of aspirin may...
T75721	ATI-2341 TFA
	ATI-2341是一种针对C-X-C趋化因子受体4型(CXCR4)的功能选择性变构激动剂，作为偏向配体，偏好促进Gα1而不是Gα13的激活。通过激活抑制性异源三聚体G蛋白(Gi)，ATI-2341抑制cAMP的产生并诱导钙动员，有效动员骨髓多形核中性粒细胞(PMNs)与造血干细胞及其祖细胞(HSPCs)。
T37166	RCTR1
	Resolvin conjugate in tissue regeneration 1 (RCTR1) is a specialized pro-resolving mediator (SPM) biosynthesized from docosahexaenoic acid by isolated human macrophages and apoptotic polymorphonuclear (PMN) neutrophils.1It has been found in human spleen and bone marrow.2RCTR1 is produced via lipoxygenase-mediated oxidation of DHA to 7(S)-8-epoxy-17(S)-HDHA, which is conjugated to glutathione.1,2,3RCTR1 (10 nM) increases phagocytosis ofE. colior apoptotic neutrophils in isolated human monocyte-de...
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...
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...
T36423	Leukotriene B5
	Leukotriene B5 (LTB5) is a leukotriene with diverse biological activities. It is a metabolite of eicosapentaenoic acid formed through the 5-lipoxygenase (5-LO) pathway. LTB5 increases contraction of bullfrog lung strips ex vivo in a concentration-dependent manner. In vivo, LTB5 (100 nM) reduces tumor volume in mice injected with Tm1 murine melanoma cells. LTB5 also elicits chemokinesis and lysosomal enzyme release from polymorphonuclear leukocytes (PMNLs) 20- to 30-fold less, and induces platele...
T38043	Resolvin E4
	Resolvin E4 (RvE4) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acid by 15-lipoxygenase (15-LO)via15(S)-HpEPE and 15S-hydroxy, 5S-HpEPE intermediatesin vitroand by isolated human M2 macrophages or polymorphonuclear (PMN) neutrophils under normoxic or hypoxic conditions. RvE4 synthesis is enhanced in M2 macrophage and neutrophil co-cultures, indicating transcellular biosynthesis by a potential 15-LO and 5-LO mechanism...
T35946	17(R)-Resolvin D1 Aspirin-triggered Resolvin D1,17(R)-Resolvin D1
	Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid.[1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D1 is produced physiologically from the sequential oxygenation of DHA by 15- and 5-lipoxygenase.[1] 17(R)-RvD1 is an aspirin-triggered epimer of RvD1 that reduces human polymorphonuclear leukocyte (PMN) transendothelial migration, the ear...
T83669	PMX-53 TFA AcPhe-[Orn-Pro-D-Cyclohexylalanine-Trp-Arg],AcF-[OPdChaWR],3D53
	PMX-53是一种大环型补体5a (C5a) 类肽模拟物及C5a受体的拮抗剂（IC50 = 0.3 µM）。它能抑制C5a诱导的人类分离性多形核白细胞（PMNs）中的髓过氧化物酶（MPO）分泌。在大鼠腹膜亚瑟斯反应模型中，PMX-53（10 mg/kg, p.o.）能够抑制血管渗漏、多形核白细胞浸润以及腹膜TNF-α和IL-6的产生。在3-硝基丙酸（3-NP）诱导的亨廷顿病大鼠模型中，它能减少体重损失和厌食，抑制纹状体退化。PMX-53（3 mg/kg）还能在ApoE-/-小鼠中减小动脉粥样硬化斑块大小和脂质含量。
T35836	PMX-205 (trifluoroacetate salt)
	PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Rela...

化合物

L-Leucyl-L-Leucine methyl ester hydrochloride

Cat.No: T7739

Synonym: Leu-Leu-ome hydrochloride

Target: Others, Endogenous Metabolite

Cat.No: T27026

Synonym: CJ 13610,CJ-13610

Target: Lipoxygenase

Cat.No: T68166

Target: Others

Cat.No: T22946

Synonym: LY 255283

Target: Leukotriene Receptor

H-Leu-Leu-OMe . HBr

Cat.No: T36879L

Synonym: H-Leu-Leu-OMe . HBr (16689-14-8 Free base)

Target: Others

Cat.No: T68166L

Synonym: Traxanox TFA(58712-69-9 Free base)

Target: Others

Aseanostatin P5

Cat.No: T69110

Cat.No: T24305

Synonym: L651,142,L651142,L-651,142,L 651,142,L-651142

Cat.No: T24328

Synonym: L680,833,L680833,L-680,833,L 680,833,L-680833

Cat.No: T22526

Synonym: 5(S),6(R)-7-trihydroxymethyl Heptanoate

Target: Others

Cat.No: T71025

Cat.No: T27408

Synonym: Gea3162,Gea-3162

Meclofenamate sodium hydrate

Cat.No: T0260L

Synonym: INF 4668,CI583,CI-583,INF-4668,CI 583,INF4668

Cat.No: TP2395

Cat.No: T15825

Target: Retinoid Receptor

Cat.No: T37460

Synonym: Lipoxin B4

Lipoxin B4 methyl ester

Cat.No: T38308

Cat.No: T21962

17(R)-Protectin D1

Cat.No: T36043

Synonym: 17(R)-Protectin D1

Cat.No: T74650

1,2,3-Trieicosapentaenoyl-rac-glycerol

Cat.No: T37382

Resolvin D1 methyl ester

Cat.No: T37168

Synonym: Resolvin D1 methyl ester

13(S)-HODE-biotin

Cat.No: T37975

MeOSuc-AAPV-pNA

Cat.No: T38363

5(S),12(S)-DiHETE

Cat.No: T37649

Traxanox sodium

Cat.No: T34917

Synonym: Y 12141,Y12141,Y-12141

14,15-dehydro Leukotriene B4

Cat.No: T37260

Synonym: 14,15-dehydro Leukotriene B4

C2 Phytoceramide (t18:0/2:0)

Cat.No: T36671

Cat.No: T37259

Defensin HNP-3 (human) (trifluoroacetate salt)

Cat.No: T38103

ATI-2341 TFA (1337878-62-2 free base)

Cat.No: TP1354

Synonym: ATI-2341 TFA

15(R)-Lipoxin A4

Cat.No: T37265

Synonym: 15(R)-Lipoxin A4,AT-Lipoxin A4

Cat.No: T75721

Cat.No: T37166

Flufenamic Acid-d4

Cat.No: T71303

Cat.No: T35881

Cat.No: T36423

Cat.No: T38043

17(R)-Resolvin D1

Cat.No: T35946

Synonym: Aspirin-triggered Resolvin D1,17(R)-Resolvin D1

Cat.No: T83669

Synonym: AcPhe-[Orn-Pro-D-Cyclohexylalanine-Trp-Arg],AcF-[OPdChaWR],3D53

PMX-205 (trifluoroacetate salt)

Cat.No: T35836

Cat. No.	Product Name	Target	Signaling Pathways
T4S1422	Praeruptorin E 白花前胡素 E,白花前胡素E	Others; Calcium Channel	Membrane transporter/Ion channel; Metabolism; Others
	Praeruptorin E 是白花前胡中的一种主要成分，是钙拮抗剂，pD2′值为 5.2。
TN4486	Magnolianin	Others	Others
	Magnolianin can inhibit strongly (IC50 = 0.45 uM) 5-HETE formation by die cytosol of guinea pig polymorphonuclear leukocytes.
TN2552	1-Methyl-2-nonylquinolin-4(1H)-one	Others	Others
	1-Methyl-2-nonylquinolin-4(1H)-one has anti-inflammatory activity, it exhibits inhibitory activity on leukotriene biosynthesis in a bioassay using human polymorphonuclear granulocytes, with IC50 values of 12.1 microM.
T13716	(+)-Guaiacin	Others	Others
	(+)-Guaiacin is a compound isolated from the bark of Machilus wangchiana Chun. It shows potent in vitro activities against the release of β-glucuronidase in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor (PAF).
TN6057	1-Methyl-2-[(Z)-6-undecenyl]-4(1H)-quinolone (Z)-1-Methyl-2-(undec-6-enyl)quinolin-4(1H)-one
	(Z)-1-Methyl-2-(undec-6-enyl)quinolin-4(1H)-one shows strong inhibitory activity on leukotriene biosynthesis in human polymorphonuclear granulocytes, and it is very effective against mycobacteria.
T79951	Piperkadsin A	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	Piperkadsin A作为一种ROS抑制剂，能够有效地抑制PMA诱导的人多形核中性粒细胞中ROS的生成，其IC50值为4.3 μM。
TN4584	Morolic acid	IL Receptor; COX; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Morolic acid and moronic acid have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1. Moro

天然产物

Cat.No: T4S1422

Synonym: 白花前胡素 E,白花前胡素E

Target: Others, Calcium Channel

Cat.No: TN4486

Target: Others

1-Methyl-2-nonylquinolin-4(1H)-one

Cat.No: TN2552

Target: Others

Cat.No: T13716

Target: Others

1-Methyl-2-[(Z)-6-undecenyl]-4(1H)-quinolone

Cat.No: TN6057

Synonym: (Z)-1-Methyl-2-(undec-6-enyl)quinolin-4(1H)-one

Cat.No: T79951

Target: Reactive Oxygen Species

Cat.No: TN4584

Target: IL Receptor, COX, HIV Protease

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