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19

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T13865 Resorcinolnaphthalein

RAAS Endocrinology/Hormones
Resorcinolnaphthalein 是一种特异性的血管紧张素转换酶 2 激活剂,EC50=19.5 μM。Resorcinolnaphthalein 能够用于高血压和肾纤维化的研究
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。
T4583 PFI-2 hydrochloride

(R)-PFI-2 hydrochloride,PFI-2 HCl

Histone Methyltransferase Chromatin/Epigenetic
PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) 是一种有效的、高度选择性的、具有细胞活性的 SETD7 甲基转移酶抑制剂,IC50值为2nM,活性是 (S)-PFI-2 的 500 倍。
T16708 R-268712

ALK; TGF-beta/Smad Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
R-268712 是选择性的 ALK5 抑制剂(IC50:2.5 nM)。
T1987 PFI-2

PFI2,PFI 2,(R)-PFI-2

Histone Methyltransferase Chromatin/Epigenetic
PFI-2 是一种有效、特异性和细胞活性的赖氨酸甲基转移酶 SETD7 抑制剂,Ki 和 IC50值分别为 0.33 和 2 nM。
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 .
T9953 BT173

Others Others
BT173 是一种新型的同源域相互作用蛋白激酶 2 (HIPK2) 抑制剂,通过抑制 TGF-β1/Smad3 通路减轻肾纤维化。
T16886 Sinefungin

Adenosyl-Ornithine,西奈芬净,A-9145,Antibiotic 32232RP

Others; Histone Methyltransferase; Antibiotic; Antifungal Chromatin/Epigenetic; Microbiology/Virology; Others
Sinefungin (Adenosyl-Ornithine) 是病毒粒子mRNA (鸟嘌呤-7-)-甲基转移酶、 mRNA (核苷-2'-)-甲基转移酶和病毒增殖的有效抑制剂。它还抑制SET7/9,通过抑制H3K4甲基化来改善肾纤维化。
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。
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。
T80072 Des-Arg9-[Leu8]-Bradykinin acetate

Bradykinin Receptor GPCR/G Protein
Des-Arg9-[Leu8]-Bradykinin acetate 是一种B1R(缓激肽受体1)拮抗剂,主要应用于肾纤维化的研究。
T79516 BT424

Src Angiogenesis; Tyrosine Kinase/Adaptors
BT424是一种特异性HCK抑制剂,能够调节体外巨噬细胞的活化及自噬,并在UUO模型中改善炎症和肾纤维化。
T70932 L6H9

L6H9 is a novel inhibitor of myeloid differentiation factor 2 (MD2), suppressing HG-induced expression of ACE and AT1 receptor and Angiotensin II (AngII) production in renal NRK‐52E cells, resulting in the decrease in fibrosis markers such as TGF-β and collagen IV.
T73088 Mavodelpar

HPP593,REN001,REN001 ; HPP593

Mavodelpar (REN001) 是一种选择性的 PPARδ激动剂。Mavodelpar 抑制肾小球损伤和肾纤维化。Mavodelpar 可用于原发性线粒体肌病 (PMM) 和长链脂肪酸氧化障碍 (LC-FAOD) 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。
T61949 Evogliptin

Evogliptin (DA-1229) 是具有口服活性的DPP4抑制剂。Evogliptin 在小鼠模型中具有显著而持久的降糖效果。Evogliptin 通过诱导自噬抑制肝细胞的纤维化和炎症信号的产生。Evogliptin 可用于 2 型糖尿病、慢性肝脏炎症,骨质疏松症及肾功能损害的研究。
T83770 Klotho-derived Peptide 1 (56-87) (human) TFA

KP1 (56-87)

Klotho衍生肽1(KP1)(56-87)是从人类Klotho蛋白质中衍生的肽,具有扰乱TGF-β信号传导的作用。它与TGF-β受体类型1(TGFBR2)和TGF-β受体类型2(TGFBR2;Kds分别为1.41和14.6µM)结合。KP1(10 µg/ml)的预孵育抑制TGF-β在NRK-49F大鼠成纤维细胞中诱导的纤维连接蛋白和α-平滑肌肌动蛋白(α-SMA)水平的增加。在体内,KP1(每天1 mg/kg)选择性地定位于受损的肾脏,并减少血清肌酐和血尿素氮水平,这些是肾功能的标志物,同时也减少了小鼠单侧输尿管阻塞(UUO)和单侧缺血-再灌注损伤诱导的肾脏纤维化模型中的肾纤维化。
T74142 Angiotensin II human TFA

Angiotensin II human (Angiotensin II) TFA 作为肾素/血管紧张素系统中关键的生物活性肽,扮演着血管收缩剂的角色并在调节人体血压中发挥中心作用。其主要通过与 G 蛋白偶联受体 (GPCRs)、血管紧张素 II 1型受体 (AT1R) 和血管紧张素 II 2型受体 (AT2R) 的相互作用来介导效应,包括刺激交感神经系统、增加醛固酮的生物合成和肾脏功能。此外,Angiotensin II human TFA 促进血管平滑肌细胞的生长和 I 型及 III 型胶原在成纤维细胞中的合成,导致血管壁与心肌增厚及纤维化,并诱导细胞凋亡。还通过LOX-1依赖的氧化还原敏感路径诱导内皮细胞中的毛细血管形成。
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...

化合物

Resorcinolnaphthalein
Cat.No: T13865
Synonym:
Target: RAAS
Fezagepras
Cat.No: T12883
Synonym: PBI-4050,3-戊基苯乙酸,Setogepram
Target: GPR
PFI-2 hydrochloride
Cat.No: T4583
Synonym: (R)-PFI-2 hydrochloride,PFI-2 HCl
Target: Histone Methyltransferase
R-268712
Cat.No: T16708
Synonym:
Target: ALK, TGF-beta/Smad
PFI-2
Cat.No: T1987
Synonym: PFI2,PFI 2,(R)-PFI-2
Target: Histone Methyltransferase
A 839977
Cat.No: T14076
Synonym: A839977,A-839977
Target: P2X Receptor, Calcium Channel
BT173
Cat.No: T9953
Synonym:
Target: Others
Sinefungin
Cat.No: T16886
Synonym: Adenosyl-Ornithine,西奈芬净,A-9145,Antibiotic 32232RP
Target: Others, Histone Methyltransferase, Antibiotic, Antifungal
KS370G
Cat.No: T24270
Synonym: KS-370-G,KS 370 G,Caffeic Acid Phenethyl Amide
Target:
Fluorofenidone
Cat.No: T15300
Synonym: AKF-PD
Target: Others
Des-Arg9-[Leu8]-Bradykinin acetate
Cat.No: T80072
Synonym:
Target: Bradykinin Receptor
BT424
Cat.No: T79516
Synonym:
Target: Src
L6H9
Cat.No: T70932
Synonym:
Target:
Mavodelpar
Cat.No: T73088
Synonym: HPP593,REN001,REN001 ; HPP593
Target:
SGC agonist 2
Cat.No: T62909
Synonym:
Target:
Evogliptin
Cat.No: T61949
Synonym:
Target:
Klotho-derived Peptide 1 (56-87) (human) TFA
Cat.No: T83770
Synonym: KP1 (56-87)
Target:
Angiotensin II human TFA
Cat.No: T74142
Synonym:
Target:
CC 401 dihydrochloride
Cat.No: T36673
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3033 Deoxycorticosterone acetate

醋酸去氧皮质酮,DOC acetate,Cortexone acetate,11-Deoxycorticosterone acetate,醋酸脱氧皮质酮

Glucocorticoid Receptor; Endogenous Metabolite; Adrenergic Receptor Endocrinology/Hormones; GPCR/G Protein; Metabolism; Neuroscience
Deoxycorticosterone acetate (Cortexone acetate) 是肾上腺产生的类固醇激素,具有盐皮质激素活性,并作为醛固酮的前体。
T3S1227 Aristolactam I

Aristolactam,Aristololactam I,马兜铃内酰胺I,Aristololactum

Apoptosis; Caspase Apoptosis; Proteases/Proteasome
Aristolactam I (Aristololactum) 是马兜铃酸 I (AA-I) 的主要代谢产物,参与导致肾损伤的过程。它具有细胞毒性,通过诱导半胱天冬酶 3 依赖性途径中的细胞凋亡介导。
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。
T72798 Ganodermaones B

Ganodermaones B 是一种肾纤维化抑制剂,抑制 TGF-β1诱导的 collagen I 和 fibronectin 的表达。
TN3753 Dalbergioidin

Tyrosinase; ROS; Akt; PI3K; TGF-beta/Smad Cytoskeletal Signaling; Immunology/Inflammation; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
Dalbergioidin exhibits tyrosinase inhibitory activity with an IC50 of 20 mM. It shows a melanin biosynthesis inhibition zone in the culture plate of Streptomyces bikiniensis that has commonly been used as an indicator organism. Dalbergioidin protects MC3T3-E1 osteoblastic cells against H2O2-induced cell damage through activation of the PI3K/AKT/SMAD1 pathway, suggests that it may be useful in bone metabolism diseases, particularly osteoporosis. Dalbergioidin also ameliorates doxorubicin-induced ...
TMA1743 Ergosterol peroxide

ERK; VEGFR; p38 MAPK; Wnt/beta-catenin; Akt; JAK; CDK; JNK; STAT; Antifection Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Foxo3a activity by inhibiting pAKT and c-Myc and activating pro-apoptotic protein Puma and Bax to

天然产物

Deoxycorticosterone acetate
Cat.No: T3033
Synonym: 醋酸去氧皮质酮,DOC acetate,Cortexone acetate,11-Deoxycorticosterone acetate,醋酸脱氧皮质酮
Target: Glucocorticoid Receptor, Endogenous Metabolite, Adrenergic Receptor
Aristolactam I
Cat.No: T3S1227
Synonym: Aristolactam,Aristololactam I,马兜铃内酰胺I,Aristololactum
Target: Apoptosis, Caspase
Dracorhodin perchlorate
Cat.No: T2S2043
Synonym: Dracorhodin perochlorate,血竭素高氯酸盐,Dracohodin perochlorate
Target: Apoptosis, Others
Ganodermaones B
Cat.No: T72798
Synonym:
Target:
Dalbergioidin
Cat.No: TN3753
Synonym:
Target: Tyrosinase, ROS, Akt, PI3K, TGF-beta/Smad
Ergosterol peroxide
Cat.No: TMA1743
Synonym:
Target: ERK, VEGFR, p38 MAPK, Wnt/beta-catenin, Akt, JAK, CDK, JNK, STAT, Antifection
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