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29

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3133	YM-90709 YM90709,YM 90709	IL Receptor; Interleukin	Immunology/Inflammation
	YM-90709是新型的能够抑制IL-5与IL-5受体结合的拮抗剂, 。
T8462	Enoximone 依诺昔酮,烯氟酮	PDE	Metabolism
	Enoximone 是一种选择性的，具有口服活性的磷酸二酯酶 III 抑制剂，也是正性肌力血管舒张剂。它通过抑制 cGMP 抑制的 PDE 来诱导血管舒张并增加细胞内 cAMP 水平。它还表现出 PDE4抑制作用，对心肌 PDE4A 的 IC50为 21.1 μM。它用于充血性心力衰竭的研究，并具有支气管扩张，抗哮喘和抗炎作用。
T1083L	Theophylline monohydrate Quibron,茶碱一水合物	HDAC; PDE; Adenosine Receptor	Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
	Theophylline monohydrate (Quibron) 似乎抑制磷酸二酯酶和前列腺素的产生，调节钙通量和细胞内钙分布，并拮抗腺苷。茶碱是黄嘌呤的天然生物碱衍生物，从植物山茶花和小粒咖啡中分离出来。在生理上，该药剂可放松支气管平滑肌，产生血管舒张（脑血管除外），刺激中枢神经系统，刺激心肌，利尿，增加胃酸分泌；它还可以抑制炎症并改善横膈膜的收缩性。
T30819	CGP 20376 CGP-20376,CGP20376
	CGP 20376 是一种苯并噻唑化合物，是一种驱虫剂，对嗜酸性粒细胞呼吸爆发的双重剂量依赖性调节体外作用，具有抗纤特性。
T10497	Benralizumab BIW-8405,MEDI-563	Apoptosis; IL Receptor; Interleukin	Apoptosis; Immunology/Inflammation
	Benralizumab (MEDI-563) 是一种靶向白介素 5 受体 α (IL-5Rα) 单克隆抗体，通过增强抗体依赖性细胞介导的细胞毒性促使嗜酸性粒细胞快速进行反应。Benralizumab 可用于严重的嗜酸性哮喘，可用于预防慢性阻塞性肺病加重。
T22879	JNJ 10191584 maleate JNJ 10191584 maleate salt,VUF6002 maleate	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	JNJ 10191584 maleate (VUF6002 maleate) 是一种具有口服活性的选择性 H4 受体拮抗剂 (Ki = 26 nM)。 JNJ 10191584 maleate 抑制嗜酸性粒细胞和肥大细胞的趋化性(IC50 = 530 nM 和 138 nM)。
T31719	Etiprednol dicloacetate BNP 166,BNP166,BNP-166	Others	Others
	Etiprednol dicloacetate (BNP-166) 是一种具有抗炎活性的皮质类固醇，可有效降低了脂多糖刺激淋巴细胞中的细胞因子产生，并减弱了凝集素诱导的组织培养中血液单核细胞的增殖。。Etiprednol dicloacetate 抑制嗜酸性粒细胞的积累，可用于哮喘等炎症性气管疾病的研究和治疗克罗恩病。
T3520	Setipiprant KYTH-105,塞替匹仑,ACT-129968	GPR; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂，IC50为6.0 nM。
TP1597L	Secretoneurin, rat acetate Secretoneurin, rat acetate(149146-12-3 Free base)	Others	Others
	Secretoneurin, rat acetate 是一种 33 个氨基酸的多肽，由分泌粒蛋白 II (SgII) 的蛋白水解加工产生。它在体内和体外诱导大鼠纹状体中的多巴胺释放，它对单核细胞和嗜酸性粒细胞有很强的趋化作用，但对粒细胞没有。
T4674	SB297006 SB 297006	CCR	Immunology/Inflammation; Microbiology/Virology
	SB297006 是一种CCR3拮抗剂，IC50为39 nM。它能够显著抑制 CCL11 处理的神经祖细胞的增殖和神经球形成。
T26470	A1777 AA1777,AA-1777,AA 1777
	A1777, a selective 5-lipoxygenase inhibitor, reduces leukocytes proliferation without affecting the eosinophils of mast cells.
T15565	Imetit dihydrobromide VUF 8325 dihydrobromide,SKF 91105 dihydrobromide	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Imetit dihydrobromide is a high affinity and effective agonist of histamine H3 and H4 receptors (Ki: 0.3 and 2.7 nM). Imetit mimics the histamine effect in triggering a shape change in eosinophils (EC50: 25 nM).
T17099	Timapiprant sodium OC000459 sodium	Others	Others
	Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra
T37650	5(S),15(S)-DiHETE
	5(S),15(S)-DiHETE is synthesized by 15-LO from 5(S)-HETE. It potentiates the degranulation of human PMNL in response to PAF, but not fMLP, calcium ionophore A23187, or LTB4. 5(S),15(S)-DiHETE is chemotactic for eosinophils with an ED50 value of 0.3 μM.
T68474	RWJ-58643 HCl
	RWJ 58643 is a reversible beta-tryptase and trypsin inhibitor. Low-dose RWJ-58643 (100 microg) and budesonide (200 microg) significantly reduced symptoms, eosinophils and levels of IL-5 following NAC. However, higher doses of RWJ-58643 (300 and 600 microg) caused a late eosinophilia and preceding increases in IL-5 compared with placebo.
T37303	5-OxoETE 5-KETE,5-OxoETE
	5-OxoETE is a polyunsaturated keto acid formed by the oxidation of 5-HETE in human neutrophils by a specific dehydrogenase.[1] It stimulates cytosolic calcium levels in neutrophils with an EC50 value of 2 nM.[2] 5-OxoETE selectively stimulates the migration and degranulation of eosinophils and activates the MAPK pathway in stimulated neutrophils via a specific G protein-coupled receptor.[3],[4],[5],[6]
T80882	Val-Gly-Ser-Glu NSC 350591
	Val-Gly-Ser-Glu (NSC 350591) 是一种ECF-A四肽。该化合物能剂量依赖性地提升人类嗜酸性粒细胞的数量，而不影响中性粒细胞的数量，并可与补体包被的绵羊红细胞(EAC3b)形成玫瑰花结。
T37273	BLX3887
	BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).1 It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 nM). BLX3887 inhibits the production of 15-LO metabolites selectively in eosinophils over neutrophils when used at a concentration of 10 μM. It also inhibits endocytosis in, and the migration of, isolated human peripheral blood mononuclear cell-derived dendritic cells in vitro. \|1...
T60366	Epinastine
	Epinastine (WAL801) 是一种抗组胺剂和肥大细胞稳定剂。Epinastine 是一种有效的，选择性的，口服活性的组胺 H1 受体 (histamine H1 receptor) 拮抗剂。Epinastine 还抑制人嗜酸性粒细胞释放 IL-8 并具有抗过敏作用。
T62604	Flunisolide hemihydrate
	Flunisolide hemihydrate 是一种皮质类固醇，是一种口服具有活力的糖皮质激素受体 (Glucocorticoid receptor) 激活剂，具有抗炎作用。Flunisolide hemihydrate 能够诱导嗜酸性粒细胞凋亡 (apoptosis)，能够用于研究哮喘或鼻炎、炎症。
T76869	Lirentelimab
	Lirentelimab (AK002) 是一种人源化IgG1单克隆抗体，目标为唾液酸结合Ig样凝集素8 (SIGLEC8)。该化合物通过诱导IL-5激活的嗜酸性粒细胞细胞凋亡并抑制IL-5介导的肥大细胞激活，用于嗜酸性胃炎、十二指肠炎的研究。
T36603	(±)5-HEPE
	(±)5-HEPE is produced by non-enzymatic oxidation of EPA. It contains equal amounts of 5(S)-HEPE and 5(R)-HEPE. The biological activity of (±)5-HEPE is likely mediated by one of the individual isomers, most commonly the 5(S) isomer in mammalian systems. EPA can be metabolized to 5-HEPE in human and bovine neutrophils, and human eosinophils, which is further metabolized to 5-oxoEPE and LTB5. The 5-series metabolites of EPA, namely 5-HEPE, 5-oxoEPE, and LTB5, have significantly decreased biological...
T37492	11-trans Leukotriene C4 11-trans Leukotriene C4
	11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum ...
T35955	PAR2 (1-6) amide (human) (trifluoroacetate salt) PAR2 (1-6) amide (human) (trifluoroacetate salt)
	PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide prod...
T38365	CAY10597
	The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the...
T37262	14,15-Leukotriene E4 14,15-Leukotriene E4
	Leukotrienes (LTs) are a group of acute inflammatory mediators derived from arachidonic acid in leukocytes. The majority of these metabolites are formed through the 5-lipoxygenase (5-LO) pathway. 14,15-LTE4 is a metabolite of 14,15-LTC4 and 14,15-LTD4, an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-LOs on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. These metabolites are classified as eoxins because they are formed mostly by eosinophils...
T37261	14,15-Leukotriene D4 14,15-Leukotriene D4
	14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both ...
T35453	β-Defensin-4 (human) (trifluoroacetate salt)
	β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It induces migration of monocytes in vitro when used at a concentration of 10 nM but does not affect migration of neutrophils and eosinophils. β-Defensin-4 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes. It also stimulates calcium mobilization, migration, and pro...
T83906	Tirzepatide sodium LY3298176
	Tirzepatide 是一种glucagon-like peptide 1 receptor (GLP-1R) 和 G protein-coupled receptor 119 (GPR119)的激动剂。它在表达人类GLP-1R或GPR119的HEK293细胞中诱导cAMP的产生（EC50s分别为6.54和1.01 nM）。Tirzepatide（100 nM）在表达人类GLP-1R或GPR119的HEK293细胞中诱导受体内化。在体内，Tirzepatide（每天10 nmol/kg）降低高脂饮食诱导的肥胖小鼠模型的体重、食物摄入量、血浆leptin、三酸甘油酯和free fatty acids (FFAs)水平、肝脏三酸甘油酯和血糖水平。它通过每三天给药50 nmol/kg的剂量，阻止A. alternata诱导的A. alternata挑战小鼠的支气管肺泡灌洗液（BALF）中嗜酸性粒细胞和淋巴细胞数量的增加。Tirzepatide（每三天50 nmol/kg）抑制由毒蕈碱受体激动剂methacholine (acetyl-β-methylcholine)导致的在糖尿病诱导的哮喘...

化合物

Cat.No: T3133

Synonym: YM90709,YM 90709

Target: IL Receptor, Interleukin

Cat.No: T8462

Synonym: 依诺昔酮,烯氟酮

Target: PDE

Theophylline monohydrate

Cat.No: T1083L

Synonym: Quibron,茶碱一水合物

Target: HDAC, PDE, Adenosine Receptor

Cat.No: T30819

Synonym: CGP-20376,CGP20376

Cat.No: T10497

Synonym: BIW-8405,MEDI-563

Target: Apoptosis, IL Receptor, Interleukin

JNJ 10191584 maleate

Cat.No: T22879

Synonym: JNJ 10191584 maleate salt,VUF6002 maleate

Target: Histamine Receptor

Etiprednol dicloacetate

Cat.No: T31719

Synonym: BNP 166,BNP166,BNP-166

Target: Others

Cat.No: T3520

Synonym: KYTH-105,塞替匹仑,ACT-129968

Target: GPR, Prostaglandin Receptor

Secretoneurin, rat acetate

Cat.No: TP1597L

Synonym: Secretoneurin, rat acetate(149146-12-3 Free base)

Target: Others

Cat.No: T4674

Synonym: SB 297006

Target: CCR

Cat.No: T26470

Synonym: AA1777,AA-1777,AA 1777

Imetit dihydrobromide

Cat.No: T15565

Synonym: VUF 8325 dihydrobromide,SKF 91105 dihydrobromide

Target: Histamine Receptor

Timapiprant sodium

Cat.No: T17099

Synonym: OC000459 sodium

Target: Others

5(S),15(S)-DiHETE

Cat.No: T37650

Cat.No: T68474

Cat.No: T37303

Synonym: 5-KETE,5-OxoETE

Val-Gly-Ser-Glu

Cat.No: T80882

Synonym: NSC 350591

Cat.No: T37273

Cat.No: T60366

Flunisolide hemihydrate

Cat.No: T62604

Cat.No: T76869

Cat.No: T36603

11-trans Leukotriene C4

Cat.No: T37492

Synonym: 11-trans Leukotriene C4

PAR2 (1-6) amide (human) (trifluoroacetate salt)

Cat.No: T35955

Synonym: PAR2 (1-6) amide (human) (trifluoroacetate salt)

Cat.No: T38365

14,15-Leukotriene E4

Cat.No: T37262

Synonym: 14,15-Leukotriene E4

14,15-Leukotriene D4

Cat.No: T37261

Synonym: 14,15-Leukotriene D4

β-Defensin-4 (human) (trifluoroacetate salt)

Cat.No: T35453

Tirzepatide sodium

Cat.No: T83906

Synonym: LY3298176

Cat. No.	Product Name	Target	Signaling Pathways
T1083	Theophylline Theo-24,1,3-Dimethylxanthine,茶碱	Endogenous Metabolite; HDAC; PDE; Adenosine Receptor; Autophagy	Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
	Theophylline (1,3-Dimethylxanthine) 是茶中的甲基黄嘌呤衍生物，具有利尿、平滑肌松弛、支气管扩张、心脏和中枢神经系统兴奋作用。
T37272	9(S),12(S),13(S)-TriHOME
	9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME...

天然产物

Cat.No: T1083

Synonym: Theo-24,1,3-Dimethylxanthine,茶碱

Target: Endogenous Metabolite, HDAC, PDE, Adenosine Receptor, Autophagy

9(S),12(S),13(S)-TriHOME

Cat.No: T37272

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