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19

抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T5424 Etosalamide

依托柳胺,Ethosalamide

Others Others
Etosalamide (Ethosalamide) 是一种解热缓解疼痛的试剂。它具有抗炎作用,可用于研究过敏性疾病。
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。
T0059 Diphenylpyraline hydrochloride

盐酸双苯比拉林,4-Diphenylmethoxy-1-methylpiperidine hydrochloride

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Diphenylpyraline hydrochloride (4-Diphenylmethoxy-1-methylpiperidine hydrochloride) 是一种组胺 H1 受体的拮抗剂,抑制多巴胺的吸收。它是可口服的抗组胺试剂,具有抗胆碱和抗过敏作用,可用于缓解过敏性疾病,如鼻炎、花粉热和瘙痒性皮肤疾病等。
T21060L NPC 567 acetate

NPC 567 acetate(109333-26-8 Free base)

Bradykinin Receptor GPCR/G Protein
NPC 567 acetate 是一种缓激肽 B2 拮抗剂,可用于治疗过敏性气道疾病的研究。
T16476 PF-03654746

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
PF-03654746 是组胺 H3 受体的选择性拮抗剂。 PF-03654746 提高了阿尔茨海默病的认知功效和疾病改善作用。 PF-03654746 可用于治疗过敏性鼻炎的研究。
T72031 BI 1015550

PDE Metabolism
BI 1015550 是一种具有口服活性的PDE4B 抑制剂,IC50值为 7.2 nM。BI 1015550 具有良好的安全性,在炎症、过敏疾病、肺纤维化和慢性阻塞性肺疾病 (COPD) 中有潜在应用。
T31072 CP-664511

UNII-W1AEF8025F,CP664511

CP-664511 is an alpha4beta1/ vascular cell adhesion molecule-1 (VCAM-1) inhibitor with therapeutic potential for allergic airway disease.
T70333 PM-43I

PM-43I is a potent inhibitor of both STAT5- and STAT6-dependent allergic airway disease in mice.
T13263 COX/5-LO-IN-1

Atreleuton analog

COX Immunology/Inflammation; Neuroscience
COX/5-LO-IN-1 is a cyclooxygenase and 5-lipoxygenase (5-LO) inhibitor, and used for inflammatory and allergic disease states.
T74646 PM-81I

PM-81I为一种高效STAT6抑制剂(针对SH2结构域),可显著减少STAT6的磷酸化水平。适用于研究过敏性肺病、过敏性鼻炎、慢性阻塞性肺病或癌症。
T60864 Sequifenadine

Sequifenadine 具有研究过敏症状的炎症性眼病潜力,它是一种 H1 抗组胺药。
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
T73129 STAT6-IN-1

STAT6-IN-1(化合物19a)是一种针对STAT6的SH2结构域表现出较高亲和力(IC50=0.028 µM)的STAT6抑制剂。该化合物主要用于研究过敏性肺病、过敏性鼻炎、慢性阻塞性肺病或癌症。
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.
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...
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.
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...
T70247 Clemizole sulfate

Clemizole sulfate is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine drug that was once widely used for treatment of allergic disease, was recently discovered to be a potent inhibitor (IC50, 24 nM) of the interaction between an HCV protein (NS4B) and HCV RNA. Although clemizole was widely used during the 1950s and 1960s, this was before contemporary ...
T83763 EPI-X4 TFA

Endogenous Peptide Inhibitor of CXCR4

EPI-X4是一种源于人血清白蛋白408-423氨基酸的内源性肽段,是趋化因子(C-X-C基序)受体4 (CXCR4)的拮抗剂。在0.8至1,000µM的浓度范围内,EPI-X4能抑制表达CXCR4的HEK293细胞中由趋化因子(C-X-C基序)配体12 (CXCL12)诱发的钙离子动员和受体内化。EPI-X4还能抑制CXCL12诱导的Jurkat T细胞和人类CD34+造血干细胞的迁移。体内实验中,EPI-X4(16µmol/kg)在急性过敏性气道高嗜酸性粒细胞疾病的小鼠模型中减少了Cxcr4依赖的炎症细胞气道浸润。慢性肾脏病患者尿液中EPI-X4的水平增高,并与肾小球滤过率(GFR)成反比。

化合物

Etosalamide
Cat.No: T5424
Synonym: 依托柳胺,Ethosalamide
Target: Others
TR-14035
Cat.No: T5310
Synonym: MDK-1191
Target: Integrin
Diphenylpyraline hydrochloride
Cat.No: T0059
Synonym: 盐酸双苯比拉林,4-Diphenylmethoxy-1-methylpiperidine hydrochloride
Target: Histamine Receptor
NPC 567 acetate
Cat.No: T21060L
Synonym: NPC 567 acetate(109333-26-8 Free base)
Target: Bradykinin Receptor
PF-03654746
Cat.No: T16476
Synonym:
Target: Histamine Receptor
BI 1015550
Cat.No: T72031
Synonym:
Target: PDE
CP-664511
Cat.No: T31072
Synonym: UNII-W1AEF8025F,CP664511
Target:
PM-43I
Cat.No: T70333
Synonym:
Target:
COX/5-LO-IN-1
Cat.No: T13263
Synonym: Atreleuton analog
Target: COX
PM-81I
Cat.No: T74646
Synonym:
Target:
Sequifenadine
Cat.No: T60864
Synonym:
Target:
Andolast
Cat.No: T26628
Synonym: CR2039,CR-2039,CR 2039
Target:
STAT6-IN-1
Cat.No: T73129
Synonym:
Target:
Adriforant
Cat.No: T68280
Synonym:
Target:
PMX-205 (trifluoroacetate salt)
Cat.No: T35836
Synonym:
Target:
Adriforant tartrate hydrate
Cat.No: T69918
Synonym:
Target:
Theophylline-d6
Cat.No: T71329
Synonym:
Target:
Clemizole sulfate
Cat.No: T70247
Synonym:
Target:
EPI-X4 TFA
Cat.No: T83763
Synonym: Endogenous Peptide Inhibitor of CXCR4
Target:
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。
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。
TN2511 Britannilactone diacetate

1,6-O,O-Diacetylbritannilactone

IL Receptor; PARP; ROS; MAPK; Caspase; JAK; JNK; STAT Angiogenesis; Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; JAK/STAT signaling; MAPK; Proteases/Proteasome; Stem Cells
1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airway disease as a lead compound. OODBL has anti-asthmatic activity, it reduces leukotriene C4 pro
T75499 Maceneolignan H

Maceneolignan H (Compound 8)是一种新的木脂素化合物,从肉豆蔻假种皮中分离而来。它表现为选择性CCR3拮抗剂(EC50=1.4 μM),具有研究过敏性疾病潜力。

天然产物

Ayanin
Cat.No: TN1416
Synonym:
Target: IL Receptor, P450, PARP, PDE
kuwanon G
Cat.No: T3S1612
Synonym: 桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G
Target: Phosphatase, Antibacterial, Bombesin Receptor, AChR, AChE, Glucosidase
Britannilactone diacetate
Cat.No: TN2511
Synonym: 1,6-O,O-Diacetylbritannilactone
Target: IL Receptor, PARP, ROS, MAPK, Caspase, JAK, JNK, STAT
Maceneolignan H
Cat.No: T75499
Synonym:
Target:
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