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15

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T26253 Tecastemizole

Norastemizole,R-43512,R43512,R 43512,T 1348

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Tecastemizole (R 43512) 是 H1 受体的选择性拮抗剂,是阿司咪唑的主要代谢产物,具有抗炎作用。
T21419 Diphenhydramine

苯海拉明,Debendrin,PM 255,PM255,Dabylen,Syntedril,PM-255

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Diphenhydramine (Syntedril) 是第一代具有抗胆碱能作用的H1 受体拮抗剂,它能透过血脑屏障。
T15259 Evatanepag

CP-533536 free acid,2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
Evatanepag (CP-533536 free acid) 是一种 EP2 受体选择性前列腺素 E2 (PGE2) 激动剂,可诱导局部骨形成,EC50 为 0.3 nM。它在大鼠骨折愈合模型中以单剂量局部给药时表现出愈合骨折的能力。
T21390 Fexofenadine

Carboxyterfenadine,Telfast,非索非那定,MDL 16.455,Allegra

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Fexofenadine (Carboxyterfenadine) 是一种抗组胺药物,用于治疗过敏症状,如鼻塞、花粉热和荨麻疹。与第一代抗组胺药相比,它通过血脑屏障并引起镇静的能力较差。
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。
T7084 2-Bromo-4'-hydroxyacetophenone

SHP-1 Inhibitor II,PTP Inhibitor I,α-Bromo-4-hydroxyacetophenone,4-Hydroxyphenacyl bromide,2-溴-4'-羟基苯乙酮

Phosphatase Metabolism
2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) 是一种PTP1B 的有效抑制剂,其Ki=42 μM。
T24771 SCH-336

SCH336,SCH 336

Cannabinoid Receptor GPCR/G Protein
SCH-336是一种 CB2受体激动剂(Ki-1.8 nM, EC50-2 nM),具有有效性,选择性和口服活性。SCH-336对 CB1受体也具有生物活性,对CB2受体的选择性是CB1的100倍。SCH-336能够减少鸟苷5'-3- o -(硫)三磷酸与含hCB 的膜的结合,抑制 BaF3/CB2 细胞迁移,抑制小鼠延迟型超敏反应模型中的白细胞迁移,抑制小鼠过敏模型中抗原诱导的肺嗜酸性粒细胞增多。
T28372 PF-06462894

PF 6462894,PF-6462894,PF6462894

PF-06462894 is a morpholinopyrimidone mGlu5 (mGlu5 Ki = 6 nM) with favorable properties. PF-06462894 did not show any evidence of immune activation in a mouse drug allergy model.
T71053 AHR-5333 mandelate

AHR-5333 mandelate is an anti-allergy compound which has been shown to protect against antigen-induced anaphylactic collapse and ascaris antigen-induced skin hypersensitivity. AHR-5333 mandelate has also been shown to inhibit 5-HETE, LTB4 and LTC4 synthesis.
T29545 Acamelin

Acamelin is a quinone isolated from the Australian black wood acacia melanoxylon. It is responsible for the allergy-inducing properties of the species.
T26447 A 78773

A78773,A-78773

A 78773 is a potent, selective, direct, and reversible 5-lipoxygenase inhibitor. It has activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tissues. A 78773 acts against inflamma
TQ0032L Rosiptor acetate

AQX-​1125,AQX ​1125,AQX​1125,AQX-1125 acetate

Rosiptor is a potent and selective SHIP1 activator. AQX-1125 inhibits Akt phosphorylation in SHIP1-proficient but not in SHIP1-deficient cells, reduces cytokine production in splenocytes, inhibits the activation of mast cells and inhibits human leukocyte
T81590 OVA peptide

OVA peptide,主要源于鸡蛋清,作为I类MHC(主要组织相容性复合体)分子H-2Kb(小鼠MHC的I类基因)所呈递的特定卵白蛋白Kb限制性表位。在过敏性研究领域,OVA peptide具有广泛应用。
T78641 ER-27319

Syk Angiogenesis; Tyrosine Kinase/Adaptors
ER-27319为吖啶酮衍生物,高效选择性抑制SYK,阻断其酪氨酸磷酸化和活性。本化合物阻止抗原刺激下人及大鼠肥大细胞释放过敏介质,IC50约为10 μM,适用于过敏性疾病研究。
T37604 ITK inhibitor

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminome...

化合物

Tecastemizole
Cat.No: T26253
Synonym: Norastemizole,R-43512,R43512,R 43512,T 1348
Target: Histamine Receptor
Diphenhydramine
Cat.No: T21419
Synonym: 苯海拉明,Debendrin,PM 255,PM255,Dabylen,Syntedril,PM-255
Target: Histamine Receptor
Evatanepag
Cat.No: T15259
Synonym: CP-533536 free acid,2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸
Target: Prostaglandin Receptor
Fexofenadine
Cat.No: T21390
Synonym: Carboxyterfenadine,Telfast,非索非那定,MDL 16.455,Allegra
Target: Histamine Receptor
Setipiprant
Cat.No: T3520
Synonym: KYTH-105,塞替匹仑,ACT-129968
Target: GPR, Prostaglandin Receptor
2-Bromo-4'-hydroxyacetophenone
Cat.No: T7084
Synonym: SHP-1 Inhibitor II,PTP Inhibitor I,α-Bromo-4-hydroxyacetophenone,4-Hydroxyphenacyl bromide,2-溴-4'-羟基苯乙酮
Target: Phosphatase
SCH-336
Cat.No: T24771
Synonym: SCH336,SCH 336
Target: Cannabinoid Receptor
PF-06462894
Cat.No: T28372
Synonym: PF 6462894,PF-6462894,PF6462894
Target:
AHR-5333 mandelate
Cat.No: T71053
Synonym:
Target:
Acamelin
Cat.No: T29545
Synonym:
Target:
A 78773
Cat.No: T26447
Synonym: A78773,A-78773
Target:
Rosiptor acetate
Cat.No: TQ0032L
Synonym: AQX-​1125,AQX ​1125,AQX​1125,AQX-1125 acetate
Target:
OVA peptide
Cat.No: T81590
Synonym:
Target:
ER-27319
Cat.No: T78641
Synonym:
Target: Syk
ITK inhibitor
Cat.No: T37604
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN2290 Uvaol

Endogenous Metabolite; JNK; PPAR DNA Damage/DNA Repair; MAPK; Metabolism
Uvaol 存在于橄榄和初榨橄榄油中,具有抗炎、抗增殖和血管舒张活性。
T3S1534 Secoxyloganin

断氧化马钱苷,幼枝含断氧化马钱子甙,金银花

Anti-infection Microbiology/Virology
Secoxyloganin 是从Lonicera japonicaThunb 提取得到,能够抑制血流量减少,具有抗过敏活性。
T8297 Gomisin N

Apoptosis Apoptosis
Gomisin N 是从五味子中分离得到的一种天然产物,有镇静和催眠生物活性。它具有用于治疗过敏和抑制癌症增殖和诱导细胞凋亡的潜力。
TN3000 4,2'-Dihydroxy-4'-methoxychalcone

Others Others
4,2'-Dihydroxy-4'-methoxychalcone shows allergy-preventive effects.
T80019 17-Hydroxyneomatrine

17-Hydroxyneomatrine 是一种从苦参 (Sophora flavescens) 提取的化合物,有效抑制人宫颈癌Hela细胞生长,并展现抗菌、抗过敏、抗肿瘤、抗心律失常、消肿、利尿、免疫调节等多种生物活性。
TN2517 1,7-Dihydroxy-2,3-dimethoxyxanthone

Others Others
1,7-Dihydroxy-2,3-dimethoxyxanthone may have medicinal use in the management of inflammation, asthma and allergy, it antagonises in a non competitive but, reversible manner the contractions induced by chemical inflammatory mediators in the guinea pig trac

天然产物

Uvaol
Cat.No: TN2290
Synonym:
Target: Endogenous Metabolite, JNK, PPAR
Secoxyloganin
Cat.No: T3S1534
Synonym: 断氧化马钱苷,幼枝含断氧化马钱子甙,金银花
Target: Anti-infection
Gomisin N
Cat.No: T8297
Synonym:
Target: Apoptosis
4,2'-Dihydroxy-4'-methoxychalcone
Cat.No: TN3000
Synonym:
Target: Others
17-Hydroxyneomatrine
Cat.No: T80019
Synonym:
Target:
1,7-Dihydroxy-2,3-dimethoxyxanthone
Cat.No: TN2517
Synonym:
Target: Others
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