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42

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8239	Cromoglicic acid	Others	Others
	Cromoglicic acid 可防止肥大细胞释放炎性化学物质，例如组胺。
T9926	Omalizumab	Others	Others
	Omalizumab 是针对人免疫球蛋白 E 的重组人源化单克隆抗体(KD:0.393 nM)。它能够结合人 FcγRIIb 受体(KD:6.37 uM)。它对持续性过敏性哮喘具有潜在的研究价值。
T9043	AS1810722	P450; STAT	JAK/STAT signaling; Metabolism; Stem Cells
	AS1810722 是口服有效的STAT6抑制剂，IC50为 1.9 nM。它是一种稠合双环嘧啶衍生物，对有良好的CYP3A4抑制作用，具有用于过敏性疾病，如哮喘和特应性疾病的研究潜力。
T0211	Azelastine Azelastina,Astelin,Azelastinum,氮卓斯汀	SARS-CoV; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience
	Azelastine (Azelastinum) 是一种选择性组胺 1 拮抗剂，可研究过敏性鼻炎、哮喘、糖尿病高脂血症和 SARS-CoV-2 。
T5310	TR-14035 MDK-1191	Integrin	Cytoskeletal Signaling
	TR-14035 (MDK-1191) 是一种具有口服活性的 α4β7/α4β1整合素双重抑制剂，对 α4β7和 α4β1作用的 IC50值分别为 7 和 87 nM，可用于炎症和自体免疫疾病的研究。
T0211L	Azelastine hydrochloride Optivar,Azelastine HCl,Allergodil,盐酸氮卓斯汀,Astelin	SARS-CoV; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience
	Azelastine hydrochloride (Astelin) 是一种选择性组胺 1拮抗剂，可研究过敏性鼻炎、哮喘、糖尿病高脂血症和 SARS-CoV-2 。
T0188	Fluticasone (propionate) 丙酸氟替卡松,CCI-187881,氟替卡松丙酸酯,Fluticasone propionate	Glucocorticoid Receptor; Virus Protease; Estrogen/progestogen Receptor; Phospholipase; Endogenous Metabolite	Endocrinology/Hormones; Metabolism; Microbiology/Virology
	Fluticasone propionate (CCI-187881) 是一种选择性糖皮质激素受体激动剂，是一种局部抗炎激素，亲和力KD 为 0.5 nM。具有抗病毒活性。
T15772	Lodoxamide tromethamine U-42585E	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Lodoxamide tromethamine 是一种的肥大细胞稳定剂，具有抗过敏特性，可用于治疗哮喘和过敏性结膜炎的研究。
T2270	Trans-Tranilast Tranilast trans-,反式-曲尼司特,反-曲尼司特	RAAS	Endocrinology/Hormones
	Trans-Tranilast 是抗过敏剂，可用于过敏性鼻炎、支气管哮喘和特应性皮炎的研究。
T1030	Triprolidine hydrochloride monohydrate 盐酸曲普利啶,盐酸曲普利啶一水合物,Triprolidine hydrochloride	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Triprolidine hydrochloride monohydrate 是一种组胺 H1 拮抗剂，用于过敏性鼻炎、哮喘。
T1531	Mometasone furoate 糠酸莫美他松,糠酸莫米松,Sch32088	Glucocorticoid Receptor	Endocrinology/Hormones
	Mometasone furoate (Sch32088) 是糖皮质激素受体激动剂，具有抗炎和抗过敏作用。它是皮质固醇类试剂，动物模型中，可局部应用于气道炎症、慢性皮肤湿疹、哮喘。
T68128	Picumast
	Picumast 是一种具有抗过敏活性，可被用于治疗哮喘，可能用于治疗治疗过敏性气道疾病。
T4566	Lodoxamide Lodoxamidum,洛草氨酸	GPR; Histamine Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Lodoxamide (Lodoxamidum) 是一种抗过敏药物，作为肥大细胞稳定剂，对治疗哮喘和过敏性结膜炎有效。
T2392	Nafamostat mesylate 甲磺酸萘莫司他,FUT-175	Apoptosis; Serine/threonin kinase; SARS-CoV; Serine Protease	Apoptosis; Cell Cycle/Checkpoint; Metabolism; Microbiology/Virology; Proteases/Proteasome
	Nafamostat mesylate (FUT-175) 是一种广谱丝氨酸蛋白酶抑制剂，血管舒缓素抑制剂，能抑制血液凝固。它通过降低颗粒酶活性和 CTL 细胞溶解抑制T 细胞自身反应活性，可抑制SARS-CoV-2 的激活。它还是潜在的补体抑制剂。
T11581	HSR6071	Others	Others
	HSR6071 是一种新型具有口服活性和有效性的抗过敏制剂，能抑制被动皮肤过敏反应 (PCA)。HSR6071 在大鼠实验性哮喘模型中显示出抗哮喘活性。
T2396	Ramatroban BAY u3405,雷马曲班	GPR; Prostaglandin Receptor; PPAR	DNA Damage/DNA Repair; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism
	Ramatroban (BAY u3405) 是一种血栓素 A(2) (TxA(2)) 拮抗剂，IC50为 14 nM。它还通过抑制PGD2结合从而拮抗CRTH2，IC50为113 nM。它用于治疗过敏性鼻炎，可用于治疗哮喘的研究。
T1278	Astemizole Laridal,Histaminos,Paralergin,阿司咪唑	Potassium Channel; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
	Astemizole (Laridal) 是一种长效、非镇静抗组胺药，用于治疗季节性过敏性鼻炎、哮喘、过敏性结膜炎和慢性特发性荨麻疹。它是组胺 H1 受体的拮抗剂，IC50值为 4 nM，还阻断 hERG K+通道，IC50值为 0.9 nM，具有抗胆碱能和止痒作用。
T14377	AZD5423	Glucocorticoid Receptor	Endocrinology/Hormones
	AZD5423 是可吸入的非甾体糖皮质激素受体选择性调节剂，能够有效降改善轻度过敏性哮喘患者的过敏原诱导反应。
T10208	A-69412 N-1-(Fur-3-ylethyl)-N-hydroxyurea	Lipoxygenase	Metabolism
	A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) 是一种特异性的 5-脂氧合酶 (5-LO) 的可逆抑制剂。 A-69412 能用于哮喘和溃疡性结肠炎，以及其他炎症和过敏症状的研究。
T0089	Cetirizine dihydrochloride 盐酸西替利嗪,P071,UCB P071,Cetirizine DiHCl	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Cetirizine dihydrochloride (UCB P071) 是羟嗪的羧化代谢物，是特异性口服有效的 H1 受体长效拮抗剂。它标记抗过敏特性，抑制过敏反应期间嗜酸性粒细胞趋化，可有效治疗过敏性鼻炎、确诊荨麻疹和花粉诱发的哮喘。
TP2008L	Lyn peptide inhibitor acetate Lyn peptide inhibitor acetate(222018-18-0 free base)	IL Receptor	Immunology/Inflammation
	Lyn peptide inhibitor acetate(222018-18-0 free base) 是一种有效的细胞渗透性 Lyn 偶联 IL-5 受体信号通路抑制剂，同时保持其他信号完整。它阻断 Lyn 活化并抑制 Lyn 酪氨酸激酶与 IL-3/GM-CSF/IL-5 受体的 βc 亚基的结合。它可用于哮喘、过敏和其他嗜酸性粒细胞疾病的研究。
T10437	AZD8848	TLR	Immunology/Inflammation
	AZD8848 is a selective antedrug agonist of toll-like receptor 7 (TLR7). It is developed for the research of asthma and allergic rhinitis.
T21112	Triprolidine hydrochloride 295 C 51,Pro-Entra,Entra,盐酸曲普利啶,Actidilat,Triprolidine hydrochloride anhydrous,Actidil,Pro-Actidil
	Triprolidine hydrochloride anhydrous, a Histamine H1 antagonist, is used in asthma, allergic rhinitis, and urticaria.
T26582	AIM-102
	AIM-102, a nonsteroidal, immune modulating, anti-inflammatory drug, is used potentially for the treatment of allergic asthma.
T26628	Andolast CR2039,CR-2039,CR 2039
	Andolast, also known as CR-2039, an anti-allergic agent for the treatment of bronchial asthma, chronic obstructive pulmonary disease (COPD). Andolast acts at different cellular levels to inhibit immunoglobulin E synthesis. Andolast proved to be significan
T1553	Chlorpheniramine maleate 马来酸氯苯那敏,NCI-C55265,Chlorphenamine maleate	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Chlorpheniramine maleate (NCI-C55265) 是一种组胺 H1 拮抗剂，IC50为12 nM，用于过敏反应、花粉热、鼻炎、荨麻疹和哮喘。
T68620	(R)-DOI hydrochloride
	(R)-DOI hydrochloride is a 5-HT2 receptor agonist, inhibiting TNF-α-mediated proinflammatory signaling cascades and inflammation via 5-HT2A receptor activation and preventing the development of, and inflammation associated with, acute allergic asthma.
T37386	Dihydro Montelukast
	Dihydro montelukast is a potential impurity found in commercial montelukast preparations. Montelukast (sodium salt) is a potent and selective cysteinyl leukotriene 1 (CysLT1) receptor antagonist. Formulations containing montelukast are used for the treatment of asthma as well as for the symptoms associated with allergic rhinitis.
T80131	C5a Anaphylatoxin (human)	Complement System	Immunology/Inflammation
	C5a Anaphylatoxin (human)为促炎多肽及白细胞化学引诱剂，主要应用于炎症与免疫领域研究，例如过敏性哮喘。
T68280	Adriforant
	Adriforant, also known as ZPL-3893787, PF-3893787 and ZPL-389, is a novel histamine H4 receptor antagonist. Adriforant shows an excellent in vitro profile that warrants their further investigation in relevant models of human disease. Histamine H4 receptor (H4R) has become a promising target for immuno-inflammatory diseases, such as allergic rhinitis, asthma or dermal allergies.
T71329	Theophylline-d6
	Theophylline-d6 is intended for use as an internal standard for the quantification of theophylline by GC- or LC-MS. Theophylline is an inhibitor of phosphodiesterase. It is also an adenosine A1 and A2 receptor antagonist. Theophylline induces relaxation of isolated cat bronchial smooth muscle segments precontracted with acetylcholine. It inhibits ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) eosinophil infiltration in an ovalbumin-sensitized mouse model of allergic asthma. F...
T62860	YM-341619
	YM-341619 (AS1617612) 是一种有效的、口服具有活力的 STAT6 抑制剂 (IC50: 0.70 nM)。YM-341619 能够抑制 IL-4 诱导的小鼠脾脏 T 细胞 Th2 分化，其 IC50 值为 0.28 nM，但不会影响 Th1 细胞的分化。YM-341619 是一种具有潜力的、能够用于过敏性疾病（如过敏性哮喘）研究的化合物。
T60590	Chloropyramine
	Chloropyramine 是竞争性可逆 H1 受体拮抗剂，可用于过敏性疾病的研究，例如结膜炎和支气管哮喘。Chloropyramine 表现出抗乳腺癌活性。
T69918	Adriforant tartrate hydrate
	Adriforant tartrate hydrate, also known as ZPL-3893787 tartrate hydrate, PF-3893787 tartrate hydrate and ZPL-389 tartrate hydrate, is a novel histamine H4 receptor antagonist. Adriforant tartrate hydrate shows an excellent in vitro profile that warrants their further investigation in relevant models of human disease. Histamine H4 receptor (H4R) has become a promising target for immuno-inflammatory diseases, such as allergic rhinitis, asthma or dermal allergies.
T64013	RPT193
	RPT193 是一种口服具有活力的 CCR4 抑制剂，对 Th2 炎性免疫细胞募集到炎症组织表现出抑制作用，在特应性皮炎、哮喘、过敏性炎症等疾病中发挥着重要作用。
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...
T22189	APC 366
	APC 366 是肥大细胞类胰蛋白酶 (tryptase) 的选择性抑制剂，Ki 值为7.1 μM。在羊过敏性哮喘模型中，APC 366 抑制抗原诱导的早期哮喘反应 (EAR)、晚期哮喘反应 (LAR) 和支气管高反应性 (BHR)。
T75806	Lyn peptide inhibitor TFA
	Lyn peptide inhibitor TFA 是一种有效的，可以细胞渗透的抑制剂，抑制Lyn 偶联的IL-5受体相关信号通路，同时保持其他信号的完整。Lyn peptide inhibitor TFA 可以阻断 Lyn 的激活，抑制 Lyn 酪氨酸激酶与 IL-3/GM-CSF/IL-5 受体的 βc 亚基结合。Lyn peptide inhibitor TFA 可用于哮喘、过敏等嗜酸性疾病的研究。
T37620	Leukotriene C4 methyl ester
	Leukotriene C4 (LTC4) is the parent cysteinyl-leukotriene produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute all...
T74583	Desmethylazelastine
	Desmethylazelastine是Azelastine经由细胞色素P450酶系统的氧化代谢形成的主要活性代谢物，具有97%的蛋白结合率和54小时的消除半衰期。Azelastine作为一种口服活性的组胺H1受体拮抗剂，特点是选择性高和亲和力强。它主要用于治疗过敏性鼻炎、哮喘、糖尿病高脂血症以及用于SARS-CoV-2的研究。
T35457	(±)12(13)-DiHOME (±)12(13)-DiHOME,Isoleukotoxin diol
	(±)12(13)-DiHOME is the diol form of (±)12(13)-EpOME , a cytochrome P450-derived epoxide of linoleic acid also known as isoleukotoxin. [1] It is formed from 12(13)-EpOME by soluble epoxide hydrolase (sEH) in neutrophils. [2] 12(13)-DiHOME is toxic to Sf21 cells expressing sEH and to lacZ-expressing control cells, unlike isoleukotoxin, which is only toxic to cells containing sEH.[1] [2] Levels of 12(13)-DiHOME are increased in rat spinal cord following burn injury, and it enhances cold tolerance...
T76942	Cendakimab
	Cendakimab (RPC4046; ABT 308; CC-93538)为一种选择性人源化IL-13重组单克隆抗体，对人野生型和变异型IL-13显示出高亲和力和效力。该抗体通过阻断IL-13与IL-13Rα1及IL-13Rα2的结合，抑制作用力分别在ELISA测定中的IC50值为352 pM与631 pM。Cendakimab还能识别野生型和R110Q多态变体IL-13，其结合亲和力分别为52 pM与50 pM。其显示出针对IL-13相关过敏/炎症性疾病的潜在治疗作用，如哮喘和嗜酸性粒细胞性食管炎。

化合物

Cromoglicic acid

Cat.No: T8239

Target: Others

Cat.No: T9926

Target: Others

Cat.No: T9043

Target: P450, STAT

Cat.No: T0211

Synonym: Azelastina,Astelin,Azelastinum,氮卓斯汀

Target: SARS-CoV, Histamine Receptor

Cat.No: T5310

Synonym: MDK-1191

Target: Integrin

Azelastine hydrochloride

Cat.No: T0211L

Synonym: Optivar,Azelastine HCl,Allergodil,盐酸氮卓斯汀,Astelin

Target: SARS-CoV, Histamine Receptor

Fluticasone (propionate)

Cat.No: T0188

Synonym: 丙酸氟替卡松,CCI-187881,氟替卡松丙酸酯,Fluticasone propionate

Target: Glucocorticoid Receptor, Virus Protease, Estrogen/progestogen Receptor, Phospholipase, Endogenous Metabolite

Lodoxamide tromethamine

Cat.No: T15772

Synonym: U-42585E

Target: Histamine Receptor

Trans-Tranilast

Cat.No: T2270

Synonym: Tranilast trans-,反式-曲尼司特,反-曲尼司特

Target: RAAS

Triprolidine hydrochloride monohydrate

Cat.No: T1030

Synonym: 盐酸曲普利啶,盐酸曲普利啶一水合物,Triprolidine hydrochloride

Target: Histamine Receptor

Mometasone furoate

Cat.No: T1531

Synonym: 糠酸莫美他松,糠酸莫米松,Sch32088

Target: Glucocorticoid Receptor

Cat.No: T68128

Cat.No: T4566

Synonym: Lodoxamidum,洛草氨酸

Target: GPR, Histamine Receptor

Nafamostat mesylate

Cat.No: T2392

Synonym: 甲磺酸萘莫司他,FUT-175

Target: Apoptosis, Serine/threonin kinase, SARS-CoV, Serine Protease

Cat.No: T11581

Target: Others

Cat.No: T2396

Synonym: BAY u3405,雷马曲班

Target: GPR, Prostaglandin Receptor, PPAR

Cat.No: T1278

Synonym: Laridal,Histaminos,Paralergin,阿司咪唑

Target: Potassium Channel, Histamine Receptor

Cat.No: T14377

Target: Glucocorticoid Receptor

Cat.No: T10208

Synonym: N-1-(Fur-3-ylethyl)-N-hydroxyurea

Target: Lipoxygenase

Cetirizine dihydrochloride

Cat.No: T0089

Synonym: 盐酸西替利嗪,P071,UCB P071,Cetirizine DiHCl

Target: Histamine Receptor

Lyn peptide inhibitor acetate

Cat.No: TP2008L

Synonym: Lyn peptide inhibitor acetate(222018-18-0 free base)

Target: IL Receptor

Cat.No: T10437

Target: TLR

Triprolidine hydrochloride

Cat.No: T21112

Synonym: 295 C 51,Pro-Entra,Entra,盐酸曲普利啶,Actidilat,Triprolidine hydrochloride anhydrous,Actidil,Pro-Actidil

Cat.No: T26582

Cat.No: T26628

Synonym: CR2039,CR-2039,CR 2039

Chlorpheniramine maleate

Cat.No: T1553

Synonym: 马来酸氯苯那敏,NCI-C55265,Chlorphenamine maleate

Target: Histamine Receptor

(R)-DOI hydrochloride

Cat.No: T68620

Dihydro Montelukast

Cat.No: T37386

C5a Anaphylatoxin (human)

Cat.No: T80131

Target: Complement System

Cat.No: T68280

Theophylline-d6

Cat.No: T71329

Cat.No: T62860

Cat.No: T60590

Adriforant tartrate hydrate

Cat.No: T69918

Cat.No: T64013

PMX-205 (trifluoroacetate salt)

Cat.No: T35836

Cat.No: T22189

Lyn peptide inhibitor TFA

Cat.No: T75806

Leukotriene C4 methyl ester

Cat.No: T37620

Desmethylazelastine

Cat.No: T74583

(±)12(13)-DiHOME

Cat.No: T35457

Synonym: (±)12(13)-DiHOME,Isoleukotoxin diol

Cat.No: T76942

Cat. No.	Product Name	Target	Signaling Pathways
TN1416	Ayanin	IL Receptor; P450; PARP; PDE	Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism
	Ayanin 是从Croton schiedeanus Schlecht 中分离得到的黄酮类物质。它是非选择性的磷酸二酯酶抑制剂，在呼吸道疾病中有研究的价值，如过敏性哮喘等。
TN2244	Sulfuretin 硫黄菊素	NF-κB; Autophagy	Autophagy; NF-κB
	Sulfuretin 是竞争性单酚酶和二酚酶活性抑制剂，IC50=13.64 μM。它通过抑制NF-κB 通路来抑制炎症反应。它可用于过敏性气道炎症的研究。它减少氧化应激、血小板聚集和诱变。
TMA1570	Sappanone A	NF-κB; Nrf2	Immunology/Inflammation; NF-κB
	Sappanone A 是一种高异黄烷酮，通过调节 Nrf2 和 NF-κB 表现出抗炎作用。Sappanone A 可以减轻卵清蛋白引起的哮喘中的过敏性气道炎症。
T3S1612	kuwanon G 桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G	Phosphatase; Antibacterial; Bombesin Receptor; AChR; AChE; Glucosidase	GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
	Kuwanon G (Moracenin B) 是一种从桑树中得到的黄酮类蛙皮素受体拮抗剂，具有杀菌作用。
TN3482	Bakkenolide B	NOS; COX	Immunology/Inflammation; Neuroscience
	Bakkenolide B has suppressive properties for allergic and inflammatory responses and may be utilized as a potent agent for the treatment of asthma.
T82248	Gymnoside I
	Gymnoside I（化合物1）是糖苷氧基苄基2-异丁基苹果酸，其在小鼠被动皮肤过敏反应（PCA）实验中展现出抗过敏效能。该化合物有望在哮喘、神经衰弱和慢性肝炎治疗研究中应用。

天然产物

Cat.No: TN1416

Target: IL Receptor, P450, PARP, PDE

Cat.No: TN2244

Synonym: 硫黄菊素

Target: NF-κB, Autophagy

Cat.No: TMA1570

Target: NF-κB, Nrf2

Cat.No: T3S1612

Synonym: 桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G

Target: Phosphatase, Antibacterial, Bombesin Receptor, AChR, AChE, Glucosidase

Cat.No: TN3482

Target: NOS, COX

Cat.No: T82248

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上海市静安区江场三路238号8楼