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15

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T13114 CCR2 antagonist 4

Teijin compound 1

CCR Immunology/Inflammation; Microbiology/Virology
CCR2 antagonist 4 (Teijin compound 1) 是高效的、特异性的CCR2拮抗剂,对 CCR2b 的IC50为 180 nM,抑制 MCP-1 诱导的趋化作用的 IC50为 24 nM。
T24270 KS370G

KS-370-G,KS 370 G,Caffeic Acid Phenethyl Amide

KS370G (Caffeic Acid Phenethyl Amide) 抑制 UUO 诱导的肾纤维化标志物表达。KS370G 是一种具有口服活性的降糖和心血管保护剂,可减少梗阻肾脏中胶原蛋白的沉积,并显著降低肾脏炎症趋化因子/粘附分子和单核细胞标志物的表达,改善压力过载小鼠心脏左室肥厚和功能。KS370G 可用于研究肾阻塞性肾病。
T32353 K 76 Carboxylic acid

K76 Carboxylic acid,K-76 Carboxylic acid

K 76 Carboxylic acid effectively blocks human complement from forming tumor cell chemokines.
T41086 IDR-1

IDR-1 is an antimicrobial peptide with activity against both Gram-positive and Gram-negative bacteria. This compound modulates innate immunity to counter infections while avoiding evident toxicities. Additionally, IDR-1 exhibits anti-inflammatory and anti-infective properties, increases the levels of monocyte chemokines, and reduces the release of pro-inflammatory cytokines.
T22477 (±)-AMG 487

Others Others
AMG 487 is an effective and selective antagonist of chemokine receptor 3. AMG 487 inhibited CXCR3-mediated cell migration induced by three CXCR3 chemokines, IP-10, ITAC and MIG (IC50: 8, 15 and 36 nM, respectively).
T73424 GA-O-06

GA-O-06是一种18β-Glycyrrhetinic acid衍生物,有效的抗菌及抗炎剂。它通过抑制NO、促炎细胞因子以及趋化因子来发挥抗炎效果,并对革兰氏阳性菌展现出高度的抗菌活性。
T78552 PB118

PB118是一种新型组蛋白去乙酰化酶 6(HDAC6)抑制剂,具备穿越血脑屏障的能力,可用于AD治疗。PB118 对 HDAC6 的 IC50 为 5.6 nM。
T61621 IMMH001

IMMH001, also known as SYL930, is an orally active compound that exhibits potent selectivity as an agonist for the S1P1 receptor, which is the sphingosine-1-phosphate receptor 1. This compound effectively reduces the levels of various chemokines and proinflammatory cytokines, such as IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 finds utility in research focused on rheumatoid arthritis (RA) [1] [2].
T73423 GA-O-02

GA-O-02,一种18β-Glycyrrhetinic acid衍生物,具有显著的抗菌和抗炎效果。该化合物通过抑制NO、促炎细胞因子及趋化因子来发挥其抗炎作用,并对革兰氏阳性菌显示出高度的抗菌活性。
T4411 DAMGO TFA (78123-71-4(Free base))

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
DAMGO TFA (78123-71-4(Free base)) 是Mu-opioid 受体的强效选择性激动剂。它也是镇痛药。它刺激钙激活的腺苷酸环化酶相关 cAMP 的产生。通过 TGF-beta1 表达趋化因子和趋化因子受体。增加老鼠的食物摄入量。
T36623 Antileukinate

Antileukinate is a synthetic hexapeptide with an acetylated amino terminus and an amidated carboxyl terminus that inhibits the binding of CXC chemokines to the chemokine receptor CXCR2. It inhibits IL-8 binding to neutrophils (Ki = 2.7-13 μM), prevents neutrophil chemotaxis and β-glucuronidase release, and blocks IL-8-induced skin edema in rabbits. At 53 mg/kg, antileukinate has been shown to protect mice against acute pancreatitis and associated lung injury.
T81738 Murabutide

Murabutide是一种合成的安全免疫调节剂,能够降低CD4和CCR5受体的表达,并促使β-趋化因子的高水平分泌,从而增强机体对病毒感染的非特异性防御能力。此外,Murabutide不会干扰病毒的进入过程、逆转录酶的活性或是在感染细胞的细胞质中早期前病毒DNA的形成。
T79256 DPP-4-IN-8

DPP-4-IN-8 (compound 27) 是一种高效的选择性DPP4抑制剂,具有 0.96 μM 的 Ki。该化合物能够抑制 Caco-2 和 HepG-2 细胞中的 DPP4 二肽酶活性,并剂量依赖性地降低 TNF-α、IL-6 和 IL-1β 的表达水平[1]。
T68182 3-Hydroxykynurenamine

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1/NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis ...
T37861 Talabostat

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...

化合物

CCR2 antagonist 4
Cat.No: T13114
Synonym: Teijin compound 1
Target: CCR
KS370G
Cat.No: T24270
Synonym: KS-370-G,KS 370 G,Caffeic Acid Phenethyl Amide
Target:
K 76 Carboxylic acid
Cat.No: T32353
Synonym: K76 Carboxylic acid,K-76 Carboxylic acid
Target:
IDR-1
Cat.No: T41086
Synonym:
Target:
(±)-AMG 487
Cat.No: T22477
Synonym:
Target: Others
GA-O-06
Cat.No: T73424
Synonym:
Target:
PB118
Cat.No: T78552
Synonym:
Target:
IMMH001
Cat.No: T61621
Synonym:
Target:
GA-O-02
Cat.No: T73423
Synonym:
Target:
DAMGO TFA (78123-71-4(Free base))
Cat.No: T4411
Synonym:
Target: Opioid Receptor
Antileukinate
Cat.No: T36623
Synonym:
Target:
Murabutide
Cat.No: T81738
Synonym:
Target:
DPP-4-IN-8
Cat.No: T79256
Synonym:
Target:
3-Hydroxykynurenamine
Cat.No: T68182
Synonym:
Target:
Talabostat
Cat.No: T37861
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T17214 Valencene

NSC 148969,NSC-148969,NSC148969

Others; Antioxidant; NF-κB NF-κB; Others; oxidation-reduction
Valencene (NSC-148969) 是一种从 Cyperus rotundus 中分离出来的倍半萜类化合物,是柑橘类水果和柑橘类衍生气味的香气成分。ValenceneValencene 具有抗过敏、抗炎、抗黑色素生成、和抗氧化活性。通过阻断 NF-κB 通路,Valencene 通过阻断 NF-κB 通路抑制 Th2 趋化因子和促炎性趋化因子的过度表达。
T9113 Myristicin

Myristicine,肉豆蔻醚

IL Receptor; Anti-infection; BCL; P450; PARP; 5-HT Receptor; Caspase; GABA Receptor; NO Synthase Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
Myristicin (Myristicine) 是一种在香料和伞形植物中发现的天然产物。肉豆蔻素具有抗胆碱能、抗菌和肝保护作用,还具有抗炎作用,其通过钙途径抑制dsrna 刺激的巨噬细胞中的NO、细胞因子、趋化因子和生长因子。Myristicin 可以诱导细胞凋亡,其特征是改变线粒体膜电位、细胞色素c 释放、Caspase-3激活、parp 切割和DNA 断裂。
T6677 Sophocarpine

ERK; p38 MAPK; NF-κB; TLR; COX; HER; JNK; STAT Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; MAPK; Neuroscience; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors
Sophocarpine 是一种从传统草药苦参中提取的重要生物碱。苦参具有抗病毒、抗肿瘤和抗炎等多种药理作用。它通过多种机制显著抑制癌细胞的生长,具有抗肿瘤活性。
TN5149 Tirotundin

NF-κB; COX; PPAR DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
Tirotundin is a PPARα/γ dual agonist, it exerts anti-diabetic effect through PPARγ pathway. It shows anti-inflammatory activity, it inhibits inhibit the activation of NF-kappa B, thereby, the synthesis of inflammatory mediators such as cytokines and chemo
TN3983 Ergosta-7,22-dien-3-one

NO Synthase; LTR Immunology/Inflammation
Ergosta-7,22-dien-3-one 是一种羊毛甾烷,能够从台湾灵芝的子实体中分离得到。Ergosta-7,22-dien-3-one 具有促炎特性,它能刺激一氧化氮的产生,诱导基因的表达,并诱导 J774A.1 细胞产生 TLRs、细胞因子、趋化因子和细胞粘附分子。

天然产物

Valencene
Cat.No: T17214
Synonym: NSC 148969,NSC-148969,NSC148969
Target: Others, Antioxidant, NF-κB
Myristicin
Cat.No: T9113
Synonym: Myristicine,肉豆蔻醚
Target: IL Receptor, Anti-infection, BCL, P450, PARP, 5-HT Receptor, Caspase, GABA Receptor, NO Synthase
Sophocarpine
Cat.No: T6677
Synonym:
Target: ERK, p38 MAPK, NF-κB, TLR, COX, HER, JNK, STAT
Tirotundin
Cat.No: TN5149
Synonym:
Target: NF-κB, COX, PPAR
Ergosta-7,22-dien-3-one
Cat.No: TN3983
Synonym:
Target: NO Synthase, LTR
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