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18

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0239	Lonidamine AF1890,氯尼达明,DICA,Diclondazolic Acid	Apoptosis; Hexokinase; Mitochondrial Metabolism	Apoptosis; Metabolism
	Lonidamine (Diclondazolic Acid) 是一种抗肿瘤药物，是己糖激酶、线粒体丙酮酸载体和质膜单羧酸转运蛋白抑制剂，同时也抑制线粒体复合物 II。
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。
TP1016L	Aviptadil Acetate 醋酸阿肽地尔,阿肽地尔,Vasoactive Intestinal Peptide acetate salt	RAAS; SARS-CoV	Endocrinology/Hormones; Microbiology/Virology
	Aviptadil Acetate (Vasoactive Intestinal Peptide acetate salt) 是模拟血管活性肠多肽类似物，具有血管舒张效应。它可诱导肺血管舒张并抑制血管 SMC 的增殖和血小板聚集。它可用于研究 SARS-CoV-2 引起的肺纤维化、肺动脉高压和呼吸衰竭。
T10110	3-CPs 3-Carbethoxypsoralen,3-Ethoxycarbonylpsoralen	Antibiotic	Microbiology/Virology
	3-CPs (3-Carbethoxypsoralen) 是一种博来霉素诱导的小鼠肺纤维化血清型荚膜多糖，属于补骨脂，可干扰抗体介导的细菌杀伤作用。3-CPs 可延缓博来霉素诱导的小鼠肺纤维化，可用于研究气道炎和哮喘。
T39719	Nrf2 activator-1 Nrf2 activator-1	Nrf2	Immunology/Inflammation
	Nrf2 activator-1 是一种有效的 NF-E2 相关因子 2 (Nrf2) 激活剂。Nrf2 activator-1 可用于研究包括哮喘、急性肺损伤 (ALI)、急性呼吸窘迫综合征 (ARDS) 和肺纤维化等 COPD 和其他呼吸系统疾病。
T16434	PAT-048	PDE	Metabolism
	PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in the lung fibrosis model. PAT-048 has an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma.
T61581	LasR-IN-2
	LasR-IN-2, a compound that inhibits the activity of LasR, forms hydrogen bonding with the TRY-56 residue. It finds application in the study of bacterial infection, neutropenia, severe burns, and chronic lung disease in cystic fibrosis (CF) [1].
T64141	ATX inhibitor 11
	ATX inhibitor 11 是 ATX (autotaxin) 的有效抑制剂 (IC50: 2.7 nM)。ATX inhibitor 11 能够缓解小鼠纤维化模型中纤维化组织的严重程度，有效减少纤维化生物标志物 α-SMA 的沉积。ATX inhibitor 11 能够用于研究肺纤维化。
T69517	Bexotegrast HCl
	Bexotegrast, also known as PLN-74809, is a small-molecule, dual selective inhibitor of αVβ1 / αVβ6 for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). These integrins cause upstream activation of TGF-β1 in actively fibrotic tissue. Inhibition of these integrins will block TGF-β1 activation, thereby preventing the growth of fibrotic tissue within the lung and bile ducts.
T61612	ATX inhibitor 15
	ATX inhibitor 15 (compound 30) is an indole-based carbamate derivative with a strong inhibitory effect on autotaxin (ATX), demonstrated by an IC50 of 2.17 nM. Additionally, ATX inhibitor 15 effectively inhibits ATX activity in vivo and suppresses the expression of pro-fibrotic genes. Furthermore, ATX inhibitor 15 exhibits protective effects in lung fibrosis induced by Bleomycin in mice [1].
T82938	ATUX-1215
	ATUX-1215是一种蛋白磷酸酶 2A (PP2A)的激活剂，能够在BLM治疗的动物模型中降低ERK、p38、JNK和Akt的磷酸化及IL-12p70、GM-CSF与IL1α的分泌，从而有助于减缓肺纤维化的发展。
T82314	GK444	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	GK444（Compound 15a），一种针对HDAC1/2的抑制剂，IC50分别为HDAC1和HDAC2的100 nM与92 nM。其对Caco-2细胞的IC50为4.1μM，并能下调原代正常人肺成纤维细胞中TGF-β1刺激的COL1A1 mRNA水平。此外，GK444还能抑制博来霉素诱发的小鼠肺纤维化。
T69035	Camostat free base
	Camostat, also known as FOY 305, is a serine protease inhibitor. Camostat is used in the treatment of some forms of cancer and is also effective against some viral infections, as well as inhibiting fibrosis in liver or kidney disease or pancreatitis. It is an inhibitor of the enzyme transmembrane protease, serine 2 (TMPRSS2). Inhibition of TMPRSS2 partially blocked infection by SARS-CoV and Human coronavirus NL63 in HeLa cell cultures. In vitro study showed that camostat significantly reduces...
T79380	Galectin-3/galectin-8-IN-1	Galectin	Immunology/Inflammation
	Galectin-3/galectin-8-IN-1 (Compound 53) 是抑制Galectin-3和galectin-8C末端结构域的双重抑制剂，其Kd值分别为4.12 μM和6.04 μM。该化合物有效抑制MRC-5肺成纤维细胞的迁移，可用于癌症和组织纤维化的研究。
T79381	Galectin-3/galectin-8-IN-2	Galectin	Immunology/Inflammation
	Galectin-3/galectin-8-IN-2（Compound 57）是一种针对Galectin-3和galectin-8C末端结构域的双重抑制剂，其Kd值分别为12.8 μM和2.06 μM。该化合物能够抑制MRC-5肺成纤维细胞的迁移，适用于癌症和组织纤维化研究领域。
T79489	JNK-1-IN-2	JNK	MAPK
	JNK-1-IN-2（Compound c6）是一种选择性JNK-1抑制剂，其IC50值为33.5 nM。同时，该化合物对JNK-2和JNK-3也具有抑制作用，其IC50值分别为112.9 nM和33.2 nM。通过抑制c-Jun蛋白的磷酸化，JNK-1-IN-2能够逆转肺部损伤，并且可以被应用于肺纤维化的相关研究。
T63776	PDE1-IN-4
	PDE1-IN-4 是有效的、选择性的 PDE1 (磷酸二酯酶 -1) 抑制剂，能够作用于 PDE1C (IC50: 10 nM)、PDE1A (IC50: 145 nM) 和 PDE1B (IC50: 354 nM)。PDE1-IN-4 能够调控 cAMP (3′,5′- 环磷酸腺苷) 和 cGMP (3′,5′- 环磷酸鸟苷)，表现出抗纤维化效果。PDE1-IN-4 能够抑制 TGF-β1 诱导的人肺成纤维细胞分化。PDE1-IN-4 能够用于研究特发性肺纤维化 (IPF)。
T36618	Rupatadine
	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...

化合物

Cat.No: T0239

Synonym: AF1890,氯尼达明,DICA,Diclondazolic Acid

Target: Apoptosis, Hexokinase, Mitochondrial Metabolism

GTS-21 dihydrochloride

Cat.No: T2663

Synonym: GTS 21 dihydrochloride,DMXB-A,DMBX-anabaseine

Target: 5-HT Receptor, AChR

Aviptadil Acetate

Cat.No: TP1016L

Synonym: 醋酸阿肽地尔,阿肽地尔,Vasoactive Intestinal Peptide acetate salt

Target: RAAS, SARS-CoV

Cat.No: T10110

Synonym: 3-Carbethoxypsoralen,3-Ethoxycarbonylpsoralen

Target: Antibiotic

Nrf2 activator-1

Cat.No: T39719

Synonym: Nrf2 activator-1

Target: Nrf2

Cat.No: T16434

Target: PDE

Cat.No: T61581

ATX inhibitor 11

Cat.No: T64141

Bexotegrast HCl

Cat.No: T69517

ATX inhibitor 15

Cat.No: T61612

Cat.No: T82938

Cat.No: T82314

Target: HDAC

Camostat free base

Cat.No: T69035

Galectin-3/galectin-8-IN-1

Cat.No: T79380

Target: Galectin

Galectin-3/galectin-8-IN-2

Cat.No: T79381

Target: Galectin

Cat.No: T79489

Target: JNK

Cat.No: T63776

Cat.No: T36618

Cat. No.	Product Name	Target	Signaling Pathways
T6S0105	Peiminine 贝母素乙,Zhebeinone,Fritillarine,Raddeanine,Verticinone	Others; Autophagy	Autophagy; Others
	Peiminine (Raddeanine) 是浙贝母中的一种生物碱，具有抗炎症活性。
T2S0690	Ecliptasaponin A 早莲苷 A,旱莲苷A,Echinocystic acid-3-o-glucoside	Others	Others
	Ecliptasaponin A (Echinocystic acid-3-o-glucoside) 是一种墨旱莲 (Eclipta prostrate) 中分离得到的五环三萜皂苷。其中墨旱莲是一种具有多效作用的滋补草药，如抗炎、保肝、抗氧化和免疫调节。
T5S0106	Peimisine 贝母辛,Ebeiensine	RAAS; AChR	Endocrinology/Hormones; Neuroscience
	Peimisine (Ebeiensine) 非竞争性拮抗气管平滑肌 M 受体，抑制 Ach 引起的平滑肌收缩。它兴奋 β 受体和拮抗内钙释放，促进一氧化氮释放，可舒张气管平滑肌，有平喘作用。
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。
T6S1572	Sauchinone	ERK; p38 MAPK; NF-κB	MAPK; NF-κB
	Sauchinone 是一种从Saururus chinensis 中获得的非对映异构的木脂素。它通过抑制I-κBα磷酸化和p65核易位来抑制 LPS 诱导的 iNOS，TNF-α 和 COX-2 表达。它具有抗炎和抗氧化活性。

天然产物

Cat.No: T6S0105

Synonym: 贝母素乙,Zhebeinone,Fritillarine,Raddeanine,Verticinone

Target: Others, Autophagy

Ecliptasaponin A

Cat.No: T2S0690

Synonym: 早莲苷 A,旱莲苷A,Echinocystic acid-3-o-glucoside

Target: Others

Cat.No: T5S0106

Synonym: 贝母辛,Ebeiensine

Target: RAAS, AChR

Mogroside III-E

Cat.No: TN1936

Synonym: 罗汉果皂苷ⅢE

Target: IL Receptor, TNF, TLR

Cat.No: T6S1572

Target: ERK, p38 MAPK, NF-κB

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