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24

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
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。
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。
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。
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。
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。
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。
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。
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。
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。
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.
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。
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.
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
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
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.
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 ...
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。
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。
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。
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。
T37495 Angiotensin (1-7) (acetate)

Angiotensin 1-7 (Ang-(1-7)) acetate 是RAS中的一种内源性七肽,具备心脏保护作用,主要表现为对心肌细胞的抗炎与抗纤维化活性。该化合物能抑制纯化的犬ACE活性(IC50=0.65 μM),通过降低ACE活性并促进一氧化氮释放,作为血管舒张调节的局部协同因子。此外,Angiotensin 1-7 acetate 可阻止血管紧张素Ⅱ诱发的平滑肌细胞增殖和肥大,同时对内皮细胞表现出抗血管生成和生长抑制作用。
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。

化合物

SC-43
Cat.No: T8478
Synonym:
Target: Apoptosis, Phosphatase, STAT
Malotilate
Cat.No: T6576
Synonym: Malotilatum,NKK 105,马洛替酯,Kantec
Target: Lipoxygenase
Belumosudil
Cat.No: T6867
Synonym: KD025,Rezurock,ROCK inhibitor,SLx-2119
Target: ROCK
PXS-5120A
Cat.No: T12584
Synonym:
Target: Others, Monoamine Oxidase
FT011
Cat.No: T7298
Synonym:
Target: Others
Fezagepras sodium
Cat.No: T12375
Synonym: Setogepram sodium salt,PBI-4050 sodium salt
Target: GPR
Selonsertib
Cat.No: T3350
Synonym: GS-4997
Target: Apoptosis, ASK, MAPK
24-Norursodeoxycholic acid
Cat.No: T10087
Synonym: nor-UDCA
Target: Others
Fezagepras
Cat.No: T12883
Synonym: PBI-4050,3-戊基苯乙酸,Setogepram
Target: GPR
Apamin acetate
Cat.No: TP1223L
Synonym: Apamine acetate,Apamin acetate(24345-16-2 Free base)
Target: Potassium Channel
MnTBAP chloride
Cat.No: T38164
Synonym: Mn(III)TBAP
Target:
KIRA-7
Cat.No: T15664
Synonym:
Target: Others
ML-290
Cat.No: T16101
Synonym:
Target: RXFP receptor
Belumosudil mesylate
Cat.No: T39555
Synonym: SLx-2119mesylate,KD025 mesylate
Target:
Apamin
Cat.No: TP1223
Synonym: Apamine
Target:
Naproxcinod
Cat.No: T33595
Synonym: AZD3582,Nitronaproxen,AZD-3582,Naproxen-N-butyl nitrate,HCT3012,AZD 3582
Target:
VCP746
Cat.No: T70421
Synonym:
Target:
Selonsertib HCl
Cat.No: T70622
Synonym:
Target:
Apamin TFA
Cat.No: T75746
Synonym:
Target:
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
Cat.No: T74544
Synonym:
Target:
Cortistatin 29
Cat.No: T76331
Synonym:
Target:
J-1063
Cat.No: T62301
Synonym:
Target:
Angiotensin (1-7) (acetate)
Cat.No: T37495
Synonym:
Target:
MLKL-IN-6
Cat.No: T79731
Synonym:
Target: Necroptosis
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。

天然产物

Aucubin
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
(±)-Taxifolin
Cat.No: T40080
Synonym: (±)-Dihydroquercetin
Target: Antioxidant, Tyrosinase
TargetMol Loading
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