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19

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T10425	AZ084	CCR	Immunology/Inflammation; Microbiology/Virology
	AZ084 是可口服的选择性 CCR8变构拮抗剂，其Ki 值为 0.9 nM，可研究哮喘。
T2036	6-OAU GTPL5846	GPR	Endocrinology/Hormones; GPCR/G Protein
	6-OAU (GTPL5846) 是 GPR84 的替代激动剂，在 Gqi5 嵌合体存在的情况下，在 HEK293 细胞中激活人 GPR84，在 PI 测定中 EC50 为 105 nM。
T69911	CU-6PMN
	CU-6PM is a new fluorescent RXR agonist. CU-6PMN was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay CU-6PMN enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such a...
T6243	U-73122 U73122	Phospholipase; Ferroptosis; Lipoxygenase	Apoptosis; Metabolism
	U-73122 (U73122) 是一种磷脂酶 C 和 5-脂氧合酶抑制剂，对磷脂酶 C 的 IC50值约为 1-2.1 µM。它是一种 PLC 抑制剂，可减少激动剂诱导的血小板和 PMN 中的 Ca2+ 增加。
T33431	MK-287 L680573,L 680573,L-680573
	MK-287 (L-680573) is a platelet activator (PAF) antagonist that effectively inhibates the binding of [3H]C18-PAF to human platelets, polynucleated white blood cells (PMN), and pulmonary membranes. May be used to treat asthma,
T22526	BML-111 5(S),6(R)-7-trihydroxymethyl Heptanoate	Others	Others
	inhibits leukotriene B4 (LTB4)-induced polymorphonuclear neutrophils (PMN) chemotaxis
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...
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.
T28933	TCV-309 TCV309
	TCV-309 is an inhibitor of platelet activating factor (PAF). TCV-309 reduces graft PMN infiltration and enhances early function of 24-hour-preserved rat kidneys with long warm ischemia. TCV-309 attenuates the priming effects of bronchoalveolar macrophages
TP1864	[Glu1]-Fibrinopeptide B [Glu1]-纤维蛋白肽B
	[Glu1]-Fibrinopeptide B, a derivative of fibrinopeptide B amino acid residues 1-14, originates from human fibrinopeptide B (hFpB). hFpB is a proteolytic cleavage product of the fibrinogen B beta-chain, specifically generated by thrombin, which plays a significant role in activating neutrophils (PMN), monocytes, and fibroblasts.
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)-...
T36017	PF-05381941
	PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively[1]. PF-05381941 inhibits LPS-stimulated release of TNF-αfrom human peripheralmononuclear (PMN) cells with an IC50 of 8 nM[1]. [1]. Kilty I, et al. TAK1 inhibition in the DFG-out conformation. Chem Biol Drug Des. 2013;82(5):500-505.
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...
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...
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...
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。

化合物

Cat.No: T10425

Target: CCR

Cat.No: T2036

Synonym: GTPL5846

Target: GPR

Cat.No: T69911

Cat.No: T6243

Synonym: U73122

Target: Phospholipase, Ferroptosis, Lipoxygenase

Cat.No: T33431

Synonym: L680573,L 680573,L-680573

Cat.No: T22526

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

Target: Others

17(R)-Protectin D1

Cat.No: T36043

Synonym: 17(R)-Protectin D1

Cat.No: T37460

Synonym: Lipoxin B4

Lipoxin B4 methyl ester

Cat.No: T38308

Cat.No: T28933

Synonym: TCV309

[Glu1]-Fibrinopeptide B

Cat.No: TP1864

Synonym: [Glu1]-纤维蛋白肽B

Cat.No: T37259

Cat.No: T36017

Cat.No: T37166

Flufenamic Acid-d4

Cat.No: T71303

Cat.No: T35881

17(R)-Resolvin D1

Cat.No: T35946

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

Cat.No: T38043

Cat.No: T83669

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

Cat. No.	Product Name	Target	Signaling Pathways
T4S1615	Sanggenon C 桑根酮C,桑根酮 C,Sanggenone C	NF-κB	NF-κB
	Sanggenon C (Sanggenone C) 是一种从桑属的根皮中分离得到的黄烷酮 Diels-Alder 加合物化合物。它可抑制NF-κB 活性，抑制 RAW264.7 细胞中诱导型一氧化氮合酶的表达，以及肿瘤坏死因子-α 刺激的细胞粘附和血管细胞粘附分子-1 的表达。它具有抗氧化和抗炎作用，也有抑制胰脂肪酶作用。
T16733	Resolvin E1 RvE1	Others	Others
	Resolvin E1 is an effective endogenous pro-resolving mediator of inflammation. Resolvin E1 has unique counterregulatory actions that inhibit PMN transendothelial migration. Resolvin E1 also acts as an effective inhibitor of leukocyte infiltration, dendrit

天然产物

Cat.No: T4S1615

Synonym: 桑根酮C,桑根酮 C,Sanggenone C

Target: NF-κB

Cat.No: T16733

Synonym: RvE1

Target: Others

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