30
12
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T20626 |
Esomeprazole
|
Proton pump; Cysteine Protease | Membrane transporter/Ion channel; Proteases/Proteasome |
Esomeprazole 是奥美拉唑(omeprazole) 的S-异构体,抑制溶酶体半胱氨酸蛋白酶legumain,防止癌症转移。它是一种质子泵抑制剂(PPI)。 | |||
T9195 |
SHR0302
ARQ252 |
Apoptosis; JAK | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
SHR0302 (ARQ252) 是一种具有口服活性的 JAK 抑制剂。它对 JAK1的结合力是 JAK2的 10 倍以上,是 JAK3的 77 倍,是 Tyk2的 420 倍。它抑制JAK1-STAT3磷酸化并诱导肝星状细胞凋亡,具有抗增殖和抗炎作用。 | |||
T1394 |
Ibuprofen
Brufen,(±)-Ibuprofe,布洛芬,Motrin,Advil |
COX | Immunology/Inflammation; Neuroscience |
Ibuprofen (Advil) 是一种丙酸衍生物和非甾体抗炎药 (NSAID),具有抗炎、镇痛和解热作用。它是COX-1和COX-2的抑制剂,IC50值分别为 13 和 370 μM,导致前列腺素和血栓素前体的形成减少。 | |||
T6540 |
Ibuprofen Lysine
布洛芬赖氨酸盐,Neoprofen |
COX | Immunology/Inflammation; Neuroscience |
Ibuprofen Lysine (Neoprofen) 是一种非甾体抗炎药。 | |||
T4503 |
Talniflumate
Somalgen,他尼氟酯 |
Chloride channel; COX; N-Acetylglucosaminyltransferase; Anion Exchanger | Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Talniflumate (Somalgen) 是一种钙激活氯离子通道 (hCLCA1/mCLCA3) 阻滞剂,可减少动物模型和细胞培养中的粘蛋白合成和释放。它通过抑制环氧合酶,并抑制 Cl-/HCO3- 交换活性,具有抗炎作用。它还增加了远端肠梗阻综合征囊性纤维化小鼠模型的存活率。 | |||
T2486 |
IOWH-032
IOWH032,IOWH 032 |
CFTR; Autophagy | Autophagy; Membrane transporter/Ion channel |
IOWH-032 (IOWH032) 是一种合成 CFTR 抑制剂,可用于研究治疗霍乱、腹泻和分泌性腹泻,在T84和CHO-CFTR 细胞实验中IC50为1.01 uM。 | |||
T2686L |
Esomeprazole Sodium
埃索美拉唑钠,(S)-Omeprazole sodium |
ATPase; Proton pump | Membrane transporter/Ion channel |
Esomeprazole Sodium ((S)-Omeprazole sodium) 是一种口服有效的活性质子泵抑制剂。Esomeprazole sodium 通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌,在胃食管反流疾病中有研究价值。Esomeprazole 是一种外泌体抑制剂,通过抑制 V-H+-ATPases 来阻断外泌体的释放。 | |||
T83064 | Anti-hepatic fibrosis agent 2 | ||
Fibrosis agent 2为针对Ewing肉瘤断点区域1 (EWSR1) 的特定抗纤维化化合物。 | |||
T2663 |
GTS-21 dihydrochloride
GTS 21 dihydrochloride,DMXB-A,DMBX-anabaseine |
5-HT Receptor; AChR | GPCR/G Protein; Neuroscience |
GTS-21 dihydrochloride (DMBX-anabaseine) 是一种选择性 α7 烟碱乙酰胆碱受体激动剂,具有抗炎和增强认知的活性。它也是一种拮抗剂,对人α4β2的 Ki 为20 nM,对5-HT3A 受体的 IC50为3.1 μM。 | |||
T10409 |
ATX inhibitor 5
|
PDE | Metabolism |
ATX inhibitor 5 是一种有效且具有口服活性的 autotaxin (ATX) 抑制剂(IC50 : 15.3 nM),可降低 CCl4 诱导的肝纤维化水平,具有抗肝纤维化作用,。 | |||
T14076 |
A 839977
A839977,A-839977 |
P2X Receptor; Calcium Channel | Membrane transporter/Ion channel; Metabolism; Neuroscience |
A 839977是一种选择性 P2X7 受体拮抗剂,具有抗炎和镇痛活性, 可抑制 P2X7 受体的 BzATP 诱发的钙内流,可用于研究肾纤维化 . | |||
T15647 |
Tipelukast
MN 001,KCA 757 |
Leukotriene Receptor | GPCR/G Protein |
Tipelukast (KCA 757) 是一种新型可口服的白三烯受体 (leukotriene receptor) 拮抗剂,是具有抗炎活性,可减少纤维化,下调 TIMP-1、1 型胶原蛋白。Tipelukast 可用于研究哮喘疾病。 | |||
T11411 |
GLPG1205
|
GPR; Others | Endocrinology/Hormones; GPCR/G Protein; Others |
GLPG1205是一种有效的、具有口服活性的 GPR84(G 蛋白偶联受体)拮抗剂,具有抗炎活性 。GLPG1205显示出良好的PK/PD 特征,可用于研究肺纤维化。 | |||
T76956 |
Vixarelimab
RG-6536,RO-7622888,KPL-716 |
Interleukin | Immunology/Inflammation |
Vixarelimab (KPL-716) 是一种人源的抗 oncostatin M (OSM)单克隆抗体,对 OSM 受体的β链有亲和力,对 IL-31 和 OSM 的信号传导有抑制作用。Vixarelimab 可用于研究重度结节性痒疹和特发性肺纤维化。 | |||
T25136 |
Aztreonam lysine
Corus 1020,Corus1020,Corus-1020,Aztreonam lysinate |
||
Aztreonam lysine is an inhaled anti-pseudomonal treatment for people who have pulmonary Pseudomonas aeruginosa infection with cystic fibrosis (CF). | |||
T70622 | Selonsertib HCl | ||
Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis ... | |||
T74996 |
FXR agonist 3
|
||
FXR agonist3 是一种抗 NASH 试剂,通过激活 FXR 起作用。FXR agonist3 抑制 COL1A1、TGF-β1、α-SMA 和 TIMP1的表达,具有抗纤维化活性。FXR agonist3 显著减轻肝脏脂肪变性和炎症,改善肝纤维化水平。 | |||
T78944 |
VDR agonist 2
|
||
VDR agonist 2(化合物16i)作为VDR(vitamin D receptor)激动剂,能有效抑制TGF-β1诱导的肝星状细胞(HSC)活化,并在体外和体内展现出显著的抗肝纤维化效果。 | |||
T80526 |
L-K6L9
|
||
L-K6L9 对于囊性纤维化患者的铜绿假单胞菌 (P. aeruginosa) 表现出显著的抗菌 (antimicrobial) 活性和抗生物膜 (anti-biofilm) 能力。该化合物的抗酶解性质保证了其在体内的稳定性,且不引发细菌的耐药性。 | |||
T61586 |
TGFβ-IN-2
|
||
TGFβ-IN-2 (Compound 9d) effectively inhibits the accumulation of total collagen induced by TGF-β in NRK-49F cells, with an IC 50 value of 4.31 μM. It also suppresses the in vitro protein expression of COL1A1, α-SMA, and p-Smad3, which are induced by TGF-β. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [1]. | |||
T64008 |
Thi-DPPY
|
||
Thi-DPPY 是一种有效的、口服具有活力的 JAK3 抑制剂,能够作用于 BTK (IC50: 62.4 nM)、JAK (IC50: 1.38 nM)。Thi-DPPY 能够抗 HBE 细胞的增殖。Thi-DPPY 在体内具有抗炎作用。Thi-DPPY 对特发性肺纤维化(IPF)表现出研究潜力。 | |||
T62301 |
J-1063
|
||
J-1063 是一种选择性、口服具有活力的、有效的 ALK5 抑制剂 (IC50: 0.039 μM)。 J-1063 能够抑制炎症浸润,胶原沉积,肝细胞坏死,表现出抗肝纤维化作用。J-1063 具有潜力进行肝纤维化的研究。 | |||
T73155 |
BMS-986339
|
||
BMS-986339 是一种具有口服活性的FXR 激动剂。BMS-986339 可与 His298 和 ASN287 残基形成氢键。BMS-986339 可用于原发性胆汁性肝硬化 (PBC)、原发性硬化性胆管炎 (PSC)、非酒精性脂肪性肝炎 (NASH),和抗纤维化研究。 | |||
T10964L |
DB1976 dihydrochloride
DB1976 hydrochloride,DB1976 2HCl |
Apoptosis; NF-κB | Apoptosis; NF-κB |
DB1976 dihydrochloride (DB1976 2HCl) ,一种转录因子 PU.1 抑制剂,具有潜在抗炎活性,可在体内实验中减缓小鼠的炎症和纤维化,改善了葡萄糖稳态和血脂异常。DB1976 dihydrochloride 促进细胞凋亡,可用于研究代谢功能障碍和非酒精性脂肪性肝炎。 | |||
T36408 |
Rhein-13C4
Rhein-13C4 |
||
Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically i... | |||
T79731 |
MLKL-IN-6
|
Necroptosis | Apoptosis |
MLKL-IN-6(compound P28)是一种针对Mixed Lineage Kinase domain-like(MLKL)的混合谱系激酶抑制剂,具有抗纤维化的潜力。它能够抑制MLKL的磷酸化和寡聚化,从而抑制细胞坏死、免疫细胞死亡,并减少粘附因子的表达。MLKL-IN-6展现出低细胞毒性,并可抑制肝星状细胞的激活,从而降低肝纤维化标志物的水平。 | |||
T71303 |
Flufenamic Acid-d4
|
||
Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear... | |||
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,... | |||
T36673 | CC 401 dihydrochloride | ||
High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 |Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J... | |||
T36618 |
Rupatadine
|
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Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6569 |
Mimosine
Leucenine,NSC 69188,含羞草素,Leucenol,L-Mimosine |
Others | Others |
Mimosine (Leucenol) 是一种酪氨酸类似物,具有抗癌和抗炎等活性。它可通过其强大的铁结合活性作为抗氧化剂,是一种 Fe(III) 螯合剂。它作用于人类白血病细胞,通过金属离子螯合、线粒体激活和诱导活性氧产生来诱导细胞凋亡。 | |||
T4S1102 |
Liensinine diperchlorate
莲心碱高氯酸盐,莲心碱二高氯酸盐,Liensinine-Perchlorate |
Mitophagy; Others; Autophagy | Autophagy; Others |
Liensinine Diperchlorate 是从芙蕖种子胚中提取的一种异喹啉生物碱。它通过阻断自噬小体-溶酶体融合来抑制晚期自噬,具有抗心律不齐、抗高血压、抗肺纤维化和血管平滑肌松弛等生物学活性。 | |||
TN1936 |
Mogroside III-E
罗汉果皂苷ⅢE |
IL Receptor; TNF; TLR | Apoptosis; Immunology/Inflammation |
Mogroside IIIe 是一种葫芦烷型化合物,从罗汉果中分离得到,可抑制 NO 的释放,具有抗肺纤维化作用。 | |||
T3795 |
Corilagin
|
Apoptosis; TLR; Reverse Transcriptase; Antibacterial; Autophagy | Apoptosis; Autophagy; Immunology/Inflammation; Microbiology/Virology |
Corilagin 是一种鞣酸,有抑制 RNA 肿瘤病毒逆转录酶的活性。它抑制金黄色葡萄球菌的生长,MIC 为 25 μg/mL。它有抗肿瘤活性,可用于肝癌和卵巢癌。 | |||
T6S1049 |
Wilforine
|
ATPase | Membrane transporter/Ion channel |
Wilforine 是一倍半萜吡啶化合物,T. wilfordii 植物中的重要生物活性化合物,可有效治疗特发性肺纤维化。它具有抗炎和杀虫活性。 | |||
TN3469 |
Aucuparin
2,6-dimethoxy-4-phenylphenol |
NADPH-oxidase | Immunology/Inflammation |
Aucuparin (2,6-dimethoxy-4-phenylphenol) 是一种植物抗菌素,具有抗炎活性。 在博来霉素 (BLM) 诱导的肺纤维化小鼠模型中,Aucuparin 抑制肺纤维化。 在经ABTS 和FRAP 测定显示出明显的清除活性。 Aucuparin 对fmlp 诱导的人中性粒细胞产生超氧化物具有明显的抑制作用,其IC50为17.0μM。 | |||
T5S0896 |
Loureirin A
龙血素 A,龙血素A |
Akt; PI3K | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Loureirin A 是一种黄酮类物质,从龙血树中分离得到,能够降低Akt 的磷酸化,具有抗血小板聚集作用。 | |||
T5S0018 |
Betulonic acid
路路通酸,(+)-Betulonic acid,Betunolic acid,Liquidambaric acid |
Parasite; HSV | Microbiology/Virology |
Betulonic acid (Liquidambaric acid) 是一种在许多植物中存在的三萜类天然产物,具有抗肿瘤,抗炎,抗寄生虫和抗病毒的活性。 | |||
T2S2043 |
Dracorhodin perchlorate
Dracorhodin perochlorate,血竭素高氯酸盐,Dracohodin perochlorate |
Apoptosis; Others | Apoptosis; Others |
Dracorhodin perchlorate 是来源于中药血竭的一种天然产物。它抑制细胞生长,并以剂量和时间依赖性方式诱导成纤维细胞凋亡,将细胞周期阻滞在 G1 期,可作为抗乳腺癌的候选药物。 | |||
T3753 |
Sinapinic Acid
Sinapic acid,芥子酸,Synapoic acid |
Apoptosis; RAAS; Reactive Oxygen Species; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Endocrinology/Hormones; Immunology/Inflammation; Metabolism; NF-κB |
Sinapinic Acid (Synapoic acid) 是从 Hydnophytum formicarumJack. 根中分离到的酚类,是HDAC 抑制剂,对ACE-I 的活性也有抑制作用。它有抗肿瘤活性,诱导肿瘤细胞凋亡,具有抗氧化、抗糖尿病的作用。 | |||
T4S0797 |
Berberine
小檗碱,Berberin,Umbellatine,黄连素 |
Reactive Oxygen Species; Topoisomerase; Endogenous Metabolite; Antibacterial; Antibiotic; Autophagy | Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB |
Berberine (Umbellatine) 是从中草药黄连中分离出来的一种生物碱抗生素。它诱导活性氧生成并抑制 DNA 拓扑异构酶,具有抗肿瘤特性。 | |||
T10554 |
Bixin
|
Others | Others |
Bixin is isolated from the seeds of Bixa orellana and possesses anti-tumor, anti-inflammatory, and antioxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation, and ROS generation. |