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Search Results for " fibrotic "

57

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16378	Ogerin	Others; 5-HT Receptor; Adenosine Receptor	GPCR/G Protein; Neuroscience; Others
	Ogerin 是选择性 GPR68正向别构调节剂(pEC50:6.83)。它能够抑制小鼠对恐惧记忆的回忆。它对 A2A 受体具有适中的拮抗作用(Ki:220 nM)。对 5-HT2B 受体的拮抗作用较弱(Ki:736 nM)。
T8478	SC-43	Apoptosis; Phosphatase; STAT	Apoptosis; JAK/STAT signaling; Metabolism; Stem Cells
	SC-43 是一种具有口服活性的SHP-1 (PTPN6)激动剂。它是Sorafenib 的衍生物，可抑制STAT3的磷酸化并诱导细胞凋亡，具有抗纤维化和抗癌作用。
T22086	HA 155 Autotaxin Inhibitor IV	PDE	Metabolism
	HA 155 (Autotaxin Inhibitor IV) 是一种基于硼酸的化合物，通过选择性结合其催化苏氨酸来抑制 ATX，IC50 为 5.7 nM。
T6576	Malotilate Malotilatum,NKK 105,马洛替酯,Kantec	Lipoxygenase	Metabolism
	Malotilate (Kantec) 是一种抗纤维化物质，是一种口服活性的促肝药，可选择性抑制5-lipoxygenase (5-LOX)(IC50=4.7 μM)。它通过降低肝脏乙醛水平并防止转铁蛋白保留在肝细胞中，从而预防了酒精-吡唑肝炎中肝细胞损伤的发展。
T6867	Belumosudil KD025,Rezurock,ROCK inhibitor,SLx-2119	ROCK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	Belumosudil (Rezurock) 是一种选择性的ROCK2抑制剂，对 ROCK1 和 ROCK2 的IC50值分别为 24 µM 和 105 nM，具有抗纤维化作用。
T22256	c-Kit-IN-5-1 3-(2-Aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one,AMG-25,3-(2-aminoquinazolin-6-yl)-4-methyl-1-[4-(1,3-oxazol-2-yl)phenyl]pyridin-2-one	c-Kit	Tyrosine Kinase/Adaptors
	c-Kit-IN-5-1 (AMG-25) 是一种新型的、高效的、选择性的 c-Kit 抑制剂。
T12584	PXS-5120A	Others; Monoamine Oxidase	Neuroscience; Others
	PXS-5120A 是一种不可逆的 Lysyl Oxidase-like 2/3 (LOXL2/3) 的氟代烯丙胺抑制剂，具有抗纤维化活性。
T7298	FT011	Others	Others
	FT011 是抗纤维化剂，能够抑制胶原蛋白 I 和 III 的 mRNA 表达，减少胶原蛋白合成。
T3350	Selonsertib GS-4997	Apoptosis; ASK; MAPK	Apoptosis; MAPK
	Selonsertib (GS-4997) 是一种选择性的，具有生物口服可利用的凋亡信号调节激酶1 抑制剂，pIC50为 8.3。它具有潜在的抗炎、抗肿瘤和抗纤维化活性。
T12375	Fezagepras sodium Setogepram sodium salt,PBI-4050 sodium salt	GPR	Endocrinology/Hormones; GPCR/G Protein
	Fezagepras sodium (Setogepram sodium salt) 是口服有效的 GPR40 激动剂及 GPR84 拮抗剂或反向激动剂。Fezagepras sodium 可以减轻肝，肾和胰腺纤维化。Fezagepras sodium 具有抗炎，抗增殖和抗纤维化作用。
T14933	Cetaben	Others	Others
	Cetaben 是不依赖 PPARα 的过氧化物酶体增殖物。它可有效降低胆固醇和甘油三酸酯的浓度，是一种非纤维化降血脂药。
T10087	24-Norursodeoxycholic acid nor-UDCA	Others	Others
	24-Norursodeoxycholic acid (nor-UDCA) 是一种侧链缩短的 UDCA 的 C23 同系物，表现出有效的抗胆汁淤积，抗炎和抗纤维化活性。
T12371L	PAT-1251	Monoamine Oxidase	Neuroscience
	PAT-1251 是一种 LOXL2 抑制剂，对小鼠、大鼠和狗的 IC50 分别为 10、0.12 和 0.16 μM，可用于纤维化疾病的研究。
T12883	Fezagepras PBI-4050,3-戊基苯乙酸,Setogepram	GPR	Endocrinology/Hormones; GPCR/G Protein
	Fezagepras (Setogepram) 是一种可口服的 GPR40激动剂和GPR84拮抗剂或反向激动剂。它减轻肾、肝和胰腺纤维化，具有抗纤维化、抗炎和抗增殖作用。
T69913	Lenumlostat PAT-1251,GB2064	Monoamine Oxidase	Neuroscience
	Lenumlostat 是一种可口服且具有选择性和有效性的赖氨酰氧化酶样蛋白 2 (LOXL2) 抑制剂，对 hLOXL2 、 hLOXL3 和 LOXL2 具有抑制作用，可用于研究纤维性疾病。
TP1223L	Apamin acetate Apamine acetate,Apamin acetate(24345-16-2 Free base)	Potassium Channel	Membrane transporter/Ion channel
	Apamin acetate (Apamine acetate) 是一种具有选择性的 Ca2+ 激活的 K+ (SK) 通道的阻断剂，是在蜂毒素中发现的一种 18 个氨基酸的肽类神经毒素。Apamin acetate 可增强皮质神经元撕裂损伤后的神经突生长和再生。Apamin acetate 具有抗炎和抗纤维化的作用。
T61389	TGFβ1-IN-1	TGF-beta/Smad	Stem Cells
	TGFβ1-IN-1 是一种具有口服活性的 TGF-β1 抑制剂，抑制 TGF-β1 诱导的纤维化标志物（α-SMA 和纤连蛋白）的产生，可用于研究癌症和自身免疫疾病。
T38164	MnTBAP chloride Mn(III)TBAP
	MnTBAP chloride (Mn(III)TBAP) 是一种具有细胞渗透性的超氧化物歧化酶 (SOD) 模拟物和过氧亚硝酸盐清除剂，能使SOD-大肠杆菌的加倍时间减少了2倍。 MnTBAP chloride 通过上调 BMPR-II 和抑制 NFκB 信号传导展现抗炎作用。MnTBAP chloride 是一种锰卟啉配合物，具有抗氧化性能，具有用于研究慢性肾脏疾病 (CKDs) 纤维化反应的潜力。
T39798	S1P2 antagonist 1
	S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist against fibrotic diseases.
T23472	Tranilast Sodium	Others	Others
	Tranilast Sodium has been used for the treatment of bronchial asthma. Tranilast is also used to autoimmune diseases, atopic and fibrotic pat.
T70382	KBP-7018 HCl
	KBP-7018 Hydrochloride is a novel, tyrosine kinase-selective inhibitor with potent effects on three fibrotic kinases (c-KIT, PDGFR, and RET).
T16101	ML-290	RXFP receptor	GPCR/G Protein
	ML-290 是一个松弛素/胰岛素样肽受体 (RXFP1) 偏向变构激动剂，为抗纤维化基因激活剂，EC50为 94 nM。
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.
T15664	KIRA-7	Others	Others
	KIRA-7 is an imidazopyrazine compound. KIRA-7 has an anti-fibrotic effect. KIRA-7 binds the IRE1α kinase (IC50: 110 nM) to allosterically inhibit its RNase activity.
T27715	KBP-7018 KBP 7018
	KBP-7018 is a potent, selective tyrosine kinase inhibitor with effects on three fibrotic kinases c-KIT, RET, and PDGFR (IC50 values are 10nM, 7.6 nM and 25nM respectively).
T33595	Naproxcinod AZD3582,Nitronaproxen,AZD-3582,Naproxen-N-butyl nitrate,HCT3012,AZD 3582
	Naproxcinod, a nitric oxide-releasing NSAID derivative, significantly improved skeletal muscle strength and fatigue resistance in sedentary and exercise mice, reducing inflammatory infiltration and fibrotic deposition in the myocardium and diaphragm. In a
T39295	Remlarsen MRG-201
	Remlarsen (MRG-201), a miR-29b mimic, functions as a miR-29b agonist with the potential to prevent the formation of fibrotic scars or cutaneous fibrosis.
T39555	Belumosudil mesylate SLx-2119mesylate,KD025 mesylate
	Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC 50 s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
TP1362	Angiogenin (108-122) Angiogenin 108-122
	Angiogenin (108-122) is an angiogenin peptide. Angiogenin (108-122) acts as a therapeutic agent for the prophylaxis and/or treatment of cancer, an infectious disease, a fibrotic disease, an inflammatory disease, a neurodegenerative disease, an autoimmune
TP1320	Angiogenin (108-122) TFA (112173-49-6 free base) Angiogenin (108-122) TFA
	Angiogenin (108-122) TFA is an angiogenin peptide.Angiogenin (108-122) acts as a therapeutic agent for the prophylaxis and/or treatment of cancer, an infectious disease, a fibrotic disease, an inflammatory disease, a neurodegenerative disease, an autoimmu
T70421	VCP746
	VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.
T79811	DDR1/2 inhibitor-2
	DDR1/2 inhibitor-2 (Example 31)，作为一种DDR1/DDR2抑制剂，其IC50值小于100 nM，适用于癌症和纤维化疾病的研究领域。
T70826	PF-03671148
	PF-03671148 is a potent ALK inhibitor. PF-03671148 inhibits the expression of fibrotic genes and protein markers both in vitro in human fibroblasts and in vivo in a rat wound repair model. Wound healing is not inhibited by the topical application of the ALK5 inhibitor to the wound. PF-03671148 may have potential utility for the prevention of dermal scarring.
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].
TP1223	Apamin Apamine
	Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity. Apamin is a bee venom compone
T80560	Tulisokibart PRA-023,PRA023
	Tulisokibart (PRA023)为人源化小鼠IgG1-κ型单克隆抗体，专一性靶向TNFSF15/TL1A。应用于炎症及纤维化疾病如克罗恩病(Crohn's Disease, CD)的研究。
T62909	SGC agonist 2
	SGC agonist 2 是一种有效的可溶性鸟苷酸环化酶 (SGC) 激动剂。其中可溶性鸟苷酸环化酶是 NO-sGC-cGMP 信号通路中的关键信号转导酶。SGC agonist 2 具有潜力进行心血管疾病 (心力衰竭、心绞痛、肺动脉高压、心肌梗塞) 和纤维化疾病 (肾纤维化、系统性硬化症) 的研究。
T76242	MMI-0100
	MMI-0100 是一种细胞渗透性肽抑制剂，抑制丝裂原活化蛋白激酶活化蛋白激酶 II (MK2)。MMI-0100 在体内外减少内膜增生。MMI-0100 抑制IL-6表达而不影响IL-8表达。MMI-0100 抑制纤维化过程，例如静脉移植疾病。
T62395	ALK5-IN-32
	ALK5-IN-32 是一种 ALK-5 的选择性抑制剂 (10 nM<IC50<100 nM)，对 TGF-β 诱导的 SMAD 信号传导也具有抑制作用。ALK5-IN-31 具有抑制体内肿瘤生长的潜力。ALK5-IN-31 可用于研究增殖性疾病（如癌症、纤维化疾病、系统性硬化症）。
T63584	ATX inhibitor 12
	ATX inhibitor 12 是口服具有活力的 ATX 抑制剂 (IC50: 1.72 nM)。在 C57Bl/6J 小鼠中，口服剂量为 60 mg/kg 的 ATX inhibitor 12 时，能够有效抑制肺结构损伤，降低纤维化病变。ATX inhibitor 12 能够用于研究特发性肺纤维化 (IPF) 。
T62676	DS89002333
	DS89002333 是一种强效的、口服具有活力的 PRKACA 抑制剂 (IC50: 0.3 nM)。DS89002333 在表达 DNAJB1-PRKACA 融合基因的 FL-HCC 患者源性异种移植模型中具有良好的抗肿瘤作用。DS89002333 能够用于研究纤维化肝细胞癌 (FL-HCC)。
T74544	(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
	(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine 是一种能同时靶向Smad3的泛素化和降解并提高HIF-α蛋白水平的双靶点PROTAC，展现出对肾性贫血的多途径抗纤维化和肾脏保护作用。
T76526	Ac-D-DGla-LI-Cha-C
	Ac-D-DGla-LI-Cha-C 是一种有效的HCV 蛋白酶抑制剂肽。Ac-D-DGla-LI-Cha-C 可用于癌症、自身免疫性疾病、纤维化疾病、炎症性疾病、神经退行性疾病、感染性疾病、肺部疾病、心脏和血管疾病以及代谢性疾病的研究。
T70275	PAT-347
	PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others.
T76331	Cortistatin 29
	Cortistatin 29，一种具备高亲和力结合至所有生长抑素(SS)受体亚型的神经肽，其对SSTR1、SSTR2、SSTR3、SSTR4、SSTR5的IC50值分别为2.8, 7.1, 0.2, 3.0, 13.7 nM。该化合物不仅能减轻神经性疼痛，还表现出抗纤维化作用。
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 ...
T78585	Pentabromopseudilin
	Pentabromopseudilin (PBrP) 为自Pseudomonas bromoutilis与Alteromonas luteoviolaceus两种海洋细菌中提取的海洋抗生素，展现抗菌、抗肿瘤及植物毒性活性。此化合物为肌球蛋白 Va(Myosin Va, MyoVa)的可逆构型抑制剂，并能有效抑制转化生长因子-β(Transforming Growth Factor-β, TGF-β)的活性，适用于纤维化疾病与癌症研究领域。
T62394	ALK5-IN-31
	ALK5-IN-31 是一种 ALK-5 的选择性抑制剂 (IC50≤10 nM)，对 TGF-β 诱导的 SMAD 信号传导也具有抑制作用。ALK5-IN-31 具有抑制体内肿瘤生长的潜力。ALK5-IN-31 可用于研究增殖性疾病（如癌症、纤维化疾病、系统性硬化症）。
T75746	Apamin TFA
	Apamin TFA (Apamine TFA) 是在蜂毒素中发现的一种 18 个氨基酸的肽类神经毒素，是一种 Ca2+激活的 K+(SK) 通道的特异性和选择性的阻断剂，具有抗炎和抗纤维化的作用。
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。

化合物

Cat.No: T16378

Target: Others, 5-HT Receptor, Adenosine Receptor

Cat.No: T8478

Target: Apoptosis, Phosphatase, STAT

Cat.No: T22086

Synonym: Autotaxin Inhibitor IV

Target: PDE

Cat.No: T6576

Synonym: Malotilatum,NKK 105,马洛替酯,Kantec

Target: Lipoxygenase

Cat.No: T6867

Synonym: KD025,Rezurock,ROCK inhibitor,SLx-2119

Target: ROCK

Cat.No: T22256

Synonym: 3-(2-Aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one,AMG-25,3-(2-aminoquinazolin-6-yl)-4-methyl-1-[4-(1,3-oxazol-2-yl)phenyl]pyridin-2-one

Target: c-Kit

Cat.No: T12584

Target: Others, Monoamine Oxidase

Cat.No: T7298

Target: Others

Cat.No: T3350

Synonym: GS-4997

Target: Apoptosis, ASK, MAPK

Fezagepras sodium

Cat.No: T12375

Synonym: Setogepram sodium salt,PBI-4050 sodium salt

Target: GPR

Cat.No: T14933

Target: Others

24-Norursodeoxycholic acid

Cat.No: T10087

Synonym: nor-UDCA

Target: Others

Cat.No: T12371L

Target: Monoamine Oxidase

Cat.No: T12883

Synonym: PBI-4050,3-戊基苯乙酸,Setogepram

Target: GPR

Cat.No: T69913

Synonym: PAT-1251,GB2064

Target: Monoamine Oxidase

Cat.No: TP1223L

Synonym: Apamine acetate,Apamin acetate(24345-16-2 Free base)

Target: Potassium Channel

Cat.No: T61389

Target: TGF-beta/Smad

MnTBAP chloride

Cat.No: T38164

Synonym: Mn(III)TBAP

S1P2 antagonist 1

Cat.No: T39798

Tranilast Sodium

Cat.No: T23472

Target: Others

Cat.No: T70382

Cat.No: T16101

Target: RXFP receptor

Bexotegrast HCl

Cat.No: T69517

Cat.No: T15664

Target: Others

Cat.No: T27715

Synonym: KBP 7018

Cat.No: T33595

Synonym: AZD3582,Nitronaproxen,AZD-3582,Naproxen-N-butyl nitrate,HCT3012,AZD 3582

Cat.No: T39295

Synonym: MRG-201

Belumosudil mesylate

Cat.No: T39555

Synonym: SLx-2119mesylate,KD025 mesylate

Angiogenin (108-122)

Cat.No: TP1362

Synonym: Angiogenin 108-122

Angiogenin (108-122) TFA (112173-49-6 free base)

Cat.No: TP1320

Synonym: Angiogenin (108-122) TFA

Cat.No: T70421

DDR1/2 inhibitor-2

Cat.No: T79811

Cat.No: T70826

ATX inhibitor 15

Cat.No: T61612

Cat.No: TP1223

Synonym: Apamine

Cat.No: T80560

Synonym: PRA-023,PRA023

Cat.No: T62909

Cat.No: T76242

Cat.No: T62395

ATX inhibitor 12

Cat.No: T63584

Cat.No: T62676

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine

Cat.No: T74544

Ac-D-DGla-LI-Cha-C

Cat.No: T76526

Cat.No: T70275

Cat.No: T76331

Selonsertib HCl

Cat.No: T70622

Pentabromopseudilin

Cat.No: T78585

Cat.No: T62394

Cat.No: T75746

Cat.No: T62301

Cat. No.	Product Name	Target	Signaling Pathways
T3416	Aucubin Aucuboside,桃叶珊瑚苷,Rhinanthin	IL Receptor; NF-κB; Antibacterial	Immunology/Inflammation; Microbiology/Virology; NF-κB
	Aucubin (Rhinanthin) 是一种可从许多传统的草药中提取的环烯醚萜苷，有许多生物学活性。
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。
T40080	(±)-Taxifolin (±)-Dihydroquercetin	Antioxidant; Tyrosinase	oxidation-reduction; Proteases/Proteasome
	(±)-Taxifolin ((±)-Dihydroquercetin) 是 Taxifolin 的外消旋体。Taxifolin 是一种常见于洋葱，水飞蓟，法国海洋松树皮和道格拉斯冷杉树皮中的类黄酮，具有抗酪氨酸酶和抗纤维化活性。Taxifolin 对胶原酶具有抑制作用，IC 50 值为 193.3 μM。Taxifolin是一种具有抗氧化能力的自由基清除剂。
T1311	4-aminobenzoic acid PABA,Vitamin H1,Vitamin Bx,para-Aminobenzoic acid,对氨基苯甲酸	Endogenous Metabolite	Metabolism
	4-aminobenzoic acid (para-Aminobenzoic acid) 是一种具有紫外线吸收和抗纤维化特性的有机酸。当暴露在光线下时，4-aminobenzoic acid 吸收紫外线并通过光化学反应释放多余的能量，这可能会对DNA造成损害。4-aminobenzoic acid 还可以增加组织水平的摄氧量，并可能增强单胺氧化酶(MAO)活性以促进血清素的降解，过量可能导致纤维化变化。

天然产物

Cat.No: T3416

Synonym: Aucuboside,桃叶珊瑚苷,Rhinanthin

Target: IL Receptor, NF-κB, Antibacterial

Mogroside III-E

Cat.No: TN1936

Synonym: 罗汉果皂苷ⅢE

Target: IL Receptor, TNF, TLR

Cat.No: T40080

Synonym: (±)-Dihydroquercetin

Target: Antioxidant, Tyrosinase

4-aminobenzoic acid

Cat.No: T1311

Synonym: PABA,Vitamin H1,Vitamin Bx,para-Aminobenzoic acid,对氨基苯甲酸

Target: Endogenous Metabolite

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