28
8
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9592 |
OATD-01
|
Others | Others |
OATD-01 是一种壳三糖苷酶及酸性哺乳动物几丁质酶的高活性抑制剂,对CHIT1具有低纳摩尔活性 (hCHIT1,IC50=23 nM)。它在多个物种中显示出良好的药代动力学特征,在体内具有显著的抗纤维化活性,可用于研究肺纤维化。 | |||
T7436 |
Cilofexor
|
FXR; Autophagy | Autophagy; Metabolism |
Cilofexor 是一种法尼醇 X 受体激动剂,EC50为 43 nM。它抑制合成肽的结合,具有抗炎和抗纤维化作用。它可用于原发性硬化性胆管炎和非酒精性脂肪性肝炎的研究。 | |||
T28578 |
Ro24-7429
Ro 24-7429,Ro-24-7429,Ro 247429 |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Ro24-7429 是一种有效的口服活性 HIV-1 反式激活蛋白 Tat 拮抗剂和一种矮小相关转录因子 1 的抑制剂。Ro24-7429 具有抗 HIV、抗纤维化和抗炎作用。 | |||
T13473 |
αvβ1 integrin-IN-1
|
Integrin | Cytoskeletal Signaling |
αvβ1 integrin-IN-1是一种强效且具有选择性的αvβ1整合素抑制剂(IC50为0.63 nM),具有抗纤维化作用。 | |||
T9947 |
GW-6604
|
PAI-1; ALK; TGF-beta/Smad | Angiogenesis; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors |
GW-6604 是一种 ALK5 抑制剂,具有明显的抗纤维化作用,可改善肝功能。 | |||
T67773 |
IMSs inhibitor S12 Perchlorate
|
Others | Others |
IMSs inhibitor S12 Perchlorate 有抗纤维化和抗癌作用。 | |||
T62882 |
Ezurpimtrostat hydrochloride
|
||
Ezurpimtrostat hydrochloride (compound 2-3) 是一种口服具有活力的抗纤维化剂,可以显著减少 DEN (二乙基亚硝胺) 肝硬化大鼠的肝纤维化。Ezurpimtrostat hydrochloride 能够用于研究纤维化、癌症、自噬和CTSB、CTSL 和 CTSD 相关疾病。 | |||
T14895 |
Tanzisertib
CC-930 |
JNK | MAPK |
Tanzisertib (CC-930) 是有效的JNK1/2/3抑制剂,IC50分别为61、7 和 6 nM。 | |||
T60162 |
1H-Pyrazole-5-carboxamide, 4-(5-chloro-2-furanyl)-1,3-bis(2,4-difluorophenyl)-4,5-dihydro-5-methyl-N-[(4-methyl-2-morpholinyl)methyl]
|
Others | Others |
1H-Pyrazole-5-carboxamide, 4-(5-chloro-2-furanyl)-1,3-bis(2,4-difluorophenyl)-4,5-dihydro-5-methyl-N-[(4-methyl-2-morpholinyl)methyl]是一种抗纤维化的化合物。 | |||
T76856 |
Andecaliximab
GS-5745 |
MMP; Virus Protease | Microbiology/Virology; Proteases/Proteasome |
Andecaliximab 是一种靶向基质金属蛋白酶 9 (MMP9) 的重组 IgG4 单克隆抗体。Andecaliximab 在特发性肺纤维化小鼠模型中显示出抗纤维化作用。Andecaliximab 可用于研究胃腺癌和特发性肺纤维化 (IPF) 以及登革热病毒。 | |||
T15300 |
Fluorofenidone
AKF-PD |
Others | Others |
Fluorofenidone (AKF-PD) 是 AMR69 的类似物,抗纤维化活性与 AMR69相同,但 Fluorofenidone 的毒性更低,半衰期长。它部分通过 PI3K/Akt 信号通路抑制 NADPH 氧化酶和细胞外基质 (ECM) 的沉积,能够减少肾间质纤维化的发生。 | |||
T39933 |
Bexotegrast
PLN-74809 |
Integrin | Cytoskeletal Signaling |
Bexotegrast (PLN-74809)是一种具有口服活性和强效性的 αvβ6和αvβ1 整合素抑制剂,具有抗纤维化作用,抑制 αvβ6 和 αvβ1 诱导的 TGF-β 激活,可用于研究特发性肺纤维化(IPF)和非特异性间质性肺炎(NSIP)。 | |||
T67961 | Safironil | Others | Others |
safironil 是一种新型抗纤维化化合物,是胶原蛋白合成的竞争性抑制剂。safironil 在体外实验中对由胶原蛋白I mRNA 或平滑肌α-actin 水平监测的成纤维细胞的激活,以及由I 型和III 型胶原蛋白和层粘连蛋白生产判断的纤维生成有抑制作用。safironil 在不改变总羟脯氨酸的情况下对肝脏肉芽肿的大小没有影响,但通过增加III 型和减少I 型胶原的沉积改变了纤维化的模式。 | |||
T10471 |
BAY 60-2770
|
Others | Others |
BAY 60-2770 is a selective and orally active soluble guanylyl cyclase (sGC) activator with antifibrotic effect. It increases the activity of sGC in a nitric oxide-independent manner. | |||
T10862 | Collagen proline hydroxylase inhibitor | Others | Others |
Collagen proline hydroxylase inhibitor is an inhibitor collagen proline hydroxylase and useful for antifibrotic proliferative agents. | |||
T40943 |
EMD527040
|
||
EMD527040 is a powerful and highly specific αvβ6 antagonist, exhibiting notable antifibrotic properties. It is suitable for conducting research on carcinoma and liver fibrosis. | |||
T68431 |
CCG-58150
|
||
CCG-58150 is a potentiInhibitor of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Response Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma. | |||
T39739 | Bersiporocin | ||
Bersiporocin, a prolyl-tRNA synthetase inhibitor, demonstrates potent activity with an IC50 of ≤100 nM against phosphoribosylpyrophosphate synthetase (PRS). This compound proves valuable for antifibrotic research. | |||
T81300 |
Relaxin H3 (human)
|
||
Relaxin H3 (human)为一类松弛素肽,通过与RXFP1受体结合来发挥其抗纤维化的生物学功能。 | |||
T12485 |
Pirfenidone-d5
AMR69 D5,Pirfenidone D5 |
Others | Others |
Pirfenidone D5 is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. | |||
T73625 | αvβ1 integrin-IN-1 TFA | ||
αvβ1integrin-IN-1 TFA (Compound C8) 为高效的αvβ1整合素选择性抑制剂,IC50值仅为0.63 nM,具备显著的抗纤维化能力。 | |||
T82165 |
HTH-02-006
|
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
HTH-02-006,一种NUAK2抑制剂(IC50 = 126 nM),能够降低HuCCT-1细胞中磷酸化MYPT1水平,并抑制YAP驱动的细胞增殖、肝肿大和肿瘤发生,同时具备抗纤维化保护效果。 | |||
T63809 |
Ansornitinib
|
||
Ansornitinib 是口服具有活力的双激酶抑制剂,能够抑制血小板衍生生长因子受体 (PDGFR) 和血管内皮生长因子受体 (VEGFR2)。Ansornitinib 是一种抗纤维化剂,能够用于研究肺部,肝脏,肾脏以及胃肠等纤维化疾病。 | |||
T74782 | CXJ-2 | PI3K | PI3K/Akt/mTOR signaling |
CXJ-2,一种环状肽,对EDP(弹性蛋白衍生肽)具中等亲和力。该化合物有效抑制PI3K/ERK通路,减少肝星状细胞的增殖与迁移,展现出显著的抗纤维化能力。 | |||
T75752 |
N-Acetyl-Ser-Asp-Lys-Pro acetate
|
||
N-Acetyl-Ser-Asp-Lys-Pro (Ac-SDKP) acetate 是血管紧张素转换酶 (ACE) N 端活性位点的特异性底物。N-Acetyl-Ser-Asp-Lys-Pro acetate 是多能干细胞增殖的天然抑制剂。N-Acetyl-Ser-Asp-Lys-Pro acetate 具有抗炎和抗纤维化特性。 | |||
T41150 |
EMD 527040 hydrochloride
|
||
EMD 527040 hydrochloride 是一种有效的整合素α V β 6抑制剂。EMD 527040 hydrochloride 对α V β 6与纤维连接蛋白的结合和表达α V β 6的细胞与纤维连接蛋白的附着有抑制作用,IC 50值分别为6 nM 和1.6 μM。EMD 527040 hydrochloride 在胆道纤维化动物模型中显示出抗纤维化活性,并在体内具有活性。 | |||
T73414 | EDP-305 | ||
EDP-305是一种具有选择性的口服farnesoid X受体(FXR)激动剂,其EC50值分别为34 nM(CHO细胞嵌合性FXR)和8 nM(HEK细胞全长FXR)。该化合物展现了强大且持久的抗纤维化效果,并适用于原发性胆道胆管炎(PBC)与非酒精性脂肪性肝炎(NASH)的研究。 | |||
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)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1738 |
Taxifolin
(+)-Taxifolin,紫杉叶素,Dihydroquercetin,二氢槲皮素,(+)-Dihydroquercetin |
VEGFR; TNF; Tyrosinase; Adrenergic Receptor; Autophagy | Angiogenesis; Apoptosis; Autophagy; GPCR/G Protein; Neuroscience; Proteases/Proteasome; Tyrosine Kinase/Adaptors |
Taxifolin (Dihydroquercetin) 是一种天然类黄酮,具有抗纤维化作用。它是一种自由基清除剂,具有抗氧化能力。它有效抑制胶原酶,IC50为 193.3 μM,具有重要的抗酪氨酸酶活性。 | |||
T2795 |
Amygdalin
苦杏仁苷,Laetrile |
Others | Others |
Amygdalin (Laetrile) 是一种植物葡萄糖苷,分离自蔷薇果实的果核中,如杏,桃,杏仁,樱桃和李子。 | |||
T3524 |
Halofuginone hydrobromide
卤夫酮溴氢酸盐,Tempostatin,RU-19110 (hydrobromide),Stenorol,常山酮溴酸盐 |
Others; Calcium Channel; DNA/RNA Synthesis; Sodium Channel; Parasite; TGF-beta/Smad | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Others; Stem Cells |
Halofuginone hydrobromid 是Febrifugine 的衍生物,是竞争性脯氨酰-tRNA 合成酶抑制剂。它是 I 型胶原合成的特异性抑制剂,并通过抑制TGF-β活性可减轻骨关节炎。它具有抗疟疾、抗炎、抗癌、抗纤维化作用。 | |||
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。 | |||
T38497 |
(-)-Taxifolin
(-)-二氢槲皮素,(-)-Dihydroquercetin |
||
(-)-Taxifolin is the less active enantiomer of Taxifolin, demonstrating vital anti-tyrosinase activity and notable inhibition against collagenase (IC50 = 193.3 μM). It is valued as an essential natural compound showing antifibrotic potential, while also acting as a capable free radical scavenger and possessing antioxidant capacity. | |||
TN3621 |
Centrolobol
|
Caspase | Apoptosis; Proteases/Proteasome |
(-)-Centrolobol has antifibrotic activity, it can significantly inhibit the proliferation of HSC-T6 cells in a dose-dependent manner. Centrolobol exhibits strong cytotoxic activity against KB cell line. | |||
T3775 |
Armepavine
亚美罂粟碱,R-Armepavine,(-)-Armepavine |
IκB/IKK; NF-κB | NF-κB |
Armepavine (R-Armepavine) 是来自Nelumbo nucifera 的活性化合物,能够抑制 TNF-α 诱导的MAPK 和NF-κB 信号级联反应。它不仅对人外周血单核细胞具有抗炎作用,且对 T 淋巴细胞和狼疮肾炎小鼠也具有免疫抑制作用。 | |||
TN4490 | Manassantin B | ERK; BCL; p38 MAPK; TNF; NF-κB; JNK; STAT; Antifection | Apoptosis; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells |
Manassantin B is a potent inhibitor of NF-κB activation by the suppression of transciptional activity of RelA/p65 subunit of NF-κB. It also possesses anti-EBV lytic replication activity. Manassantin B inhibits interleukin-6-induced signal transducer and activator of transcription 3 activation in Hep3B cells, it has potential as a potent anti-inflammatory drug for use in pathological processes such as sepsis or acute lung injury. Manassantin B exerts antifibrotic activity in HSC-T6 cells, in pa... |